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Histamine receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Histamine Receptor (545) 5-HT Receptor (68) Adenosine Receptor (1) Adenylate Cyclase (1) Adrenergic Receptor (52) Akt (10) Amino Acid Derivatives (1) Amyloid-β (7) Antibiotic (1) Apelin Receptor (APJ) (1) Apoptosis (38) Autophagy (13) Bacterial (24) Biochemical Assay Reagents (4) Calcium Channel (13) Casein Kinase (2) Caspase (4) CCR (2) CDK (1) Checkpoint Kinase (Chk) (1) Cholinesterase (ChE) (7) COX (2) CRAC Channel (1) CXCR (6) Cytochrome P450 (13) Dengue Virus (4) Dopamine Receptor (56) Dopamine Transporter (1) Drug Derivative (1) Drug Intermediate (2) Drug Isomer (3) Drug Metabolite (9) Endogenous Metabolite (27) Endothelin Receptor (1) Enterovirus (4) Epigenetic Reader Domain (1) FAK (2) FAP (1) Fc Receptor (FcR) (1) Ferroptosis (1) Filovirus (1) Flavivirus (4) Fluorescent Dye (1) FOXO (2) GABA Receptor (6) GnRH Receptor (1) HBV (4) HCV (3) HCV Protease (2) HDAC (1) Histone Methyltransferase (1) HIV (1) iGluR (3) IKK (4) Influenza Virus (9) Integrin (3) Interleukin Related (5) Isotope-Labeled Compounds (74) Keap1-Nrf2 (4) Leukotriene Receptor (3) Lipoxygenase (2) mAChR (25) Macrophage migration inhibitory factor (MIF) (1) MDM-2/p53 (2) mGluR (3) MOFs (1) Monoamine Oxidase (2) mTOR (4) Na+/Ca2+ Exchanger (3) Neurokinin Receptor (1) Neuropeptide Y Receptor (1) Neurotensin Receptor (3) NF-κB (3) NO Synthase (1) Orexin Receptor (OX Receptor) (1) P-glycoprotein (1) P2X Receptor (2) p38 MAPK (13) p62 (4) Parasite (5) PARP (1) PERK (2) Phosphatase (1) Phosphodiesterase (PDE) (4) Platelet-activating Factor Receptor (PAFR) (1) Potassium Channel (15) Prostaglandin Receptor (1) Protease Activated Receptor (PAR) (1) Pyroptosis (4) Reactive Oxygen Species (ROS) (10) Reference Standards (110) SARS-CoV (6) Serotonin Transporter (6) Sigma Receptor (9) Sodium Channel (5) STAT (1) Tau Protein (1) TNF Receptor (1) Trace Amine-associated Receptor (TAAR) (1) Transmembrane Glycoprotein (4) Trk Receptor (1) TRP Channel (5) VEGFR (3)
By Research Areas:	Cancer (102) Cardiovascular Disease (41) Endocrinology (197) Infection (37) Inflammation/Immunology (308) Metabolic Disease (60) Neurological Disease (270)
Click Chemistry:	Alkynes (1)

616

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Antibodies

Click Chemistry

Targets Recommended: Histamine Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10121

Asenapine 3 Publications Verification Org 5222	5-HT Receptor Adrenergic Receptor Dopamine Receptor Histamine Receptor	Neurological Disease
Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and **histamine receptors (pK_i**: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder .

HY-12206

Thioperamide 3 Publications Verification MR-12842	Histamine Receptor	Neurological Disease
Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a K_i of 4.3 nM for inhibition of [ ³H]histamine release. Thioperamide inhibits [ ³H]histamine synthesis with a K_i of 31 nM .

HY-B1296

Promethazine 1 Publications Verification (±)-Promethazine	Histamine Receptor	Neurological Disease Endocrinology
Promethazine is an orally active **histamine receptor** antagonist . Promethazine is first-generation antihistamine of the phenothiazine family, shows strong sedative and weak antipsychotic effects .

HY-11100

Asenapine maleate 3 Publications Verification Org 5222 maleate	5-HT Receptor	Neurological Disease
Asenapine (Org 5222) maleate, a brain-penetrant atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and **histamine receptors (pK_i**: 8.2-9.0). Asenapine maleate can be used in the research of schizophrenia and bipolar disorder .

HY-B0298

Clemastine 10+ Cited Publications HS-592; Meclastine	Histamine Receptor mAChR Autophagy Apoptosis Keap1-Nrf2 p62 mTOR Pyroptosis IKK	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Clemastine (HS-592; Meclastine) is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .

HY-B1303A

Mebhydrolin	Histamine Receptor	Inflammation/Immunology Endocrinology
Mebhydrolin is a specific **histamine H₁ receptor** antagonist.

HY-A0191

Dexbrompheniramine (+)-Brompheniramine; (S)-Brompheniramine	Endogenous Metabolite Histamine Receptor TRP Channel	Neurological Disease Metabolic Disease Inflammation/Immunology
Dexbrompheniramine ((+)-Brompheniramine; (S)-Brompheniramine) is a dual inhibitor of **histamine H1 receptor and TRPV1** receptor that can cross the blood-brain barrier. Dexbrompheniramine exerts its effects by functionally blocking H1 receptor activity and dose-dependently inhibiting TRPV1-mediated calcium responses, including Capsaicin (HY-10448)-induced responses. The combination of Dexbrompheniramine with Cimetidine (HY-14289) eliminates histamine-induced and sham-feeding-induced drinking behavior, whereas Dexbrompheniramine alone does not induce thirst or alter sham-feeding behavior in rats. Dexbrompheniramine can be used in the research of chronic cough and related pathological mechanisms .

HY-B1589A

Carbinoxamine maleate salt 1 Publications Verification	Histamine Receptor Influenza Virus	Infection Inflammation/Immunology
Carbinoxamine maleate salt is a blood-brain barrier-permeable **histamine H1 receptor** antagonist. Carbinoxamine maleate salt blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. Carbinoxamine maleate salt inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. Carbinoxamine maleate salt can be used in research on allergic rhinitis, influenza, etc.

HY-B1303

Mebhydrolin napadisylate Mebhydroline 1,5-naphthalenedisulfonate salt	Histamine Receptor	Inflammation/Immunology Endocrinology
Mebhydrolin napadisylate is a specific **histamine H₁ receptor** antagonist.

HY-107560

4-Methylhistamine dihydrochloride	Histamine Receptor	Inflammation/Immunology Cancer
4-Methylhistamine hydrochloride is the dihydrochloride salt of 4-Methylhistamine (HY-W580721). 4-Methylhistamine hydrochloride is a potent and selective agonist of **histamine 4 receptor (H4R) with a K_i** of 50 nM. 4-Methylhistamine hydrochloride has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine hydrochloride can potently activate the hH4R (pEC₅₀ = 7.4). 4-Methylhistamine hydrochloride can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation .

HY-B0160

Lafutidine FRG-8813	Histamine Receptor	Metabolic Disease Endocrinology
Lafutidine (FRG-8813) is a **histamine H2-receptor** antagonist (H₂RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease .

HY-107566

Conessine	Histamine Receptor Parasite MDM-2/p53 NF-κB FOXO Bacterial	Infection Neurological Disease
Conessine is an orally active and BBB-penetrable selective **histamine H3 receptor antagonist. The pK_i** values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy .

HY-B0426A

Olopatadine hydrochloride ALO4943A; KW4679	Histamine Receptor CXCR	Infection Neurological Disease Metabolic Disease Inflammation/Immunology
Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active **histamine H1 receptor** antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4 ⁺ and CD8 ⁺ T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis .

HY-B1478

Dimaprit dihydrochloride	Histamine Receptor NO Synthase	Endocrinology
Dimaprit dihydrochloride is a selective **histamine H2 receptor agonist, it also inhibits nNOS with an IC₅₀** of 49 μM. Dimaprit dihydrochloride can stimulate gastric acid secretion .

HY-14111

GSK189254A 2 Publications Verification GSK189254 free base	Histamine Receptor	Neurological Disease Endocrinology
GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pK_i values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.

HY-17428

Tripelennamine hydrochloride	Histamine Receptor	Neurological Disease Inflammation/Immunology
Tripelennamine hydrochloride is a histamine H1-receptor antagonist. Tripelennamine hydrochloride effectively reverses histamine-induced bronchoconstriction, increased transpulmonary pressure, elevated pulmonary vascular resistance and reduced dynamic compliance. Tripelennamine hydrochloride does not significantly affect arterial hypoxemia, hemoglobin desaturation and hypercapnia in horses undergoing short-term high-intensity exercise. Tripelennamine hydrochloride exhibits local and central analgesic activity. Tripelennamine hydrochloride can be used in studies related to emphysema, urticaria and acute laminitis .

HY-15539

Niperotidine	Histamine Receptor	Metabolic Disease Endocrinology
Niperotidine is a **histamine H2-receptor** antagonist.

HY-16567

Asenapine hydrochloride 3 Publications Verification Org 5222 hydrochloride	5-HT Receptor Dopamine Receptor Adrenergic Receptor Histamine Receptor	Neurological Disease
Asenapine (Org 5222) hydrochloride, an atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and **histamine receptors (pK_i**: 8.2-9.0). Asenapine hydrochloride can be used in the research of schizophrenia and bipolar disorder r .

HY-19365

AB-MECA 1 Publications Verification	Adenosine Receptor	Neurological Disease
AB-MECA is a high affinity A₃ adenosine receptor agonist with a binding K_i of 430.5 nM for human A₃ receptors in CHO cells. AB-MECA can enhance plasma histamine level .

HY-19443

UCB-35440	Histamine Receptor Lipoxygenase	Inflammation/Immunology
UCB-35440 is an orally active **histamine H1 receptor antagonist and 5-lipoxygenase** inhibitor. UCB-35440 can be used for the research of dermatologic inflammatory conditions .

HY-W516880

Desmethylastemizole O-Demethylastemizole	Drug Metabolite Parasite Histamine Receptor Potassium Channel	Infection Cardiovascular Disease
Desmethylastemizole (O-Demethylastemizole) , a metabolite of Astemizole (HY-12532), is a β-hematin (βH) inhibitor. Desmethylastemizole has an antiplasmodium activity against P. falciparum with IC₅₀ of 0.12, 0.11 and 0.06  μM for Pf3D7, PfDd2, and PfItG strains, respectively. Desmethylastemizole is also a **Histamine H1 receptor antagonist. Desmethylastemizole significantly blocks hERG K ⁺** channels and also inhibits histone-lysine N-methyltransferase EZH2 activity. Desmethylastemizole can be used for long QT syndrome and malaria research .

HY-W492795

Quifenadine hydrochloride	Histamine Receptor	Cardiovascular Disease
Quifenadine hydrochloride is an H1-histamine receptor blocker and can be used in the research of anti-arrhythmia .

HY-B1204S1

Histamine-d4 Ergamine-d₄	Isotope-Labeled Compounds Histamine Receptor p38 MAPK Akt Reactive Oxygen Species (ROS) Apoptosis Endogenous Metabolite	Neurological Disease Inflammation/Immunology Endocrinology Cancer
Histamine-d₄ (Ergamine-d₄) is deuterium labeled Histamine (HY-B1204). Histamine is the agonist for **histamine receptor** and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-107561

A-943931 hydrochloride	Histamine Receptor	Inflammation/Immunology
A-943931 (Compound 10) is a histamine H₄ receptor antagonists. A-943931 has improved pharmacotropic and in vivo efficacy in models of pain and inflammation. A-943931 can be used in vivo anti-inflammatory and anti-nociception research .

HY-115447

Clobenpropit	Histamine Receptor	Neurological Disease
Clobenpropit is a potent **histamine H3-receptor** antagonist. Clobenpropit decreases dopamine release and increases histamine levels in the hypothalamus. Clobenpropit shows antipsychotic-like activities. Clobenpropit causes a resuscitating effect in rats subjected to the hemorrhagic shock .

HY-107557

Proxyfan	Histamine Receptor	Neurological Disease
Proxyfan is a potent **histamine H3 receptor antagonist with K_i** values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan is over 1000-fold more potent at H3 receptors than other histamine receptors .

HY-107557A

Proxyfan Oxalate	Histamine Receptor	Neurological Disease
Proxyfan Oxalate is a potent **histamine H3 receptor antagonist with K_i** values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan Oxalate is over 1000-fold more potent at H3 receptors than other histamine receptors .

HY-A0191A

Dexbrompheniramine maleate (+)-Brompheniramine maleate; (S)-Brompheniramine maleate	TRP Channel Histamine Receptor	Inflammation/Immunology
Dexbrompheniramine ((+)-Brompheniramine; (S)-Brompheniramine) maleate is a dual inhibitor of **histamine H1 receptor and TRPV1** receptor that can cross the blood-brain barrier. Dexbrompheniramine maleate exerts its effects by functionally blocking H1 receptor activity and dose-dependently inhibiting TRPV1-mediated calcium responses, including Capsaicin (HY-10448)-induced responses. The combination of Dexbrompheniramine maleate with Cimetidine (HY-14289) eliminates histamine-induced and sham-feeding-induced drinking behavior, whereas Dexbrompheniramine maleate alone does not induce thirst or alter sham-feeding behavior in rats. Dexbrompheniramine maleate can be used in the research of chronic cough and related pathological mechanisms .

HY-W580721

4-Methylhistamine	Histamine Receptor	Inflammation/Immunology Cancer
4-Methylhistamine is a potent and selective agonist of **histamine 4 receptor (H4R) with a K_i** of 50 nM. 4-Methylhistamine has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine can potently activate the hH4R (pEC₅₀ = 7.4). 4-Methylhistamine can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation .

HY-137090

BP 2-94 BP 2.94	Histamine Receptor	Neurological Disease
BP 2-94 (BP 2.94) is an orally active and highly selective prodrug targeting the **histamine H3 receptor*. BP 2-94 exerts anti-inflammatory, analgesic and antinociceptive effects by inhibiting histamine* release and modulating neurogenic inflammation. BP 2-94 is promising for research of asthma, migraines, and inflammatory pain-related disorders .

HY-107566A

Conessine dihydrobromide	Histamine Receptor Parasite MDM-2/p53 NF-κB FOXO Bacterial	Infection Neurological Disease
Conessine dihydrobromide is an orally active and BBB-penetrable selective **histamine H3 receptor antagonist. The pK_i** values of Conessine dihydrobromide for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine dihydrobromide is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine dihydrobromide has antimalarial activity. Conessine dihydrobromide can also be used in the research of muscle atrophy .

HY-145106

Histamine H4 receptor antagonist-1	Histamine Receptor	Inflammation/Immunology
Histamine H4 receptor antagonist-1 is an antagonist of **histamine H4 receptor** extracted from patent WO2010108059A1 compound 60 .

HY-115833

Histamine H4 receptor antagonist-2	Histamine Receptor	Cancer
Histamine H4 receptor antagonist-2 serves as a potent activator of p53, demonstrating significant antitumor efficacy.

HY-B1510S

Acrivastine D7 BW825C d₇	Histamine Receptor	Inflammation/Immunology Endocrinology
Acrivastine-d₇ is a deuterium labeled Acrivastine. Acrivastine is a short acting histamine 1 receptor antagonist.

HY-107559

GT-2016	Histamine Receptor	Neurological Disease
GT-2016 is a potent, selective, and brain penetrant **histamine H3 receptor antagonist with a K_i** of 43.8 nM. GT-2016 displays selectivity against H1 and H2 receptors, and has non-active against histamine methyltransferase .

HY-107562A

JNJ-10181457	Histamine Receptor	Neurological Disease
JNJ-10181457 is a selective non-imidazole **histamine H3 receptor** antagonist that normalizes acetylcholine neurotransmission . JNJ-10181457 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-17042B

(S)-Cetirizine dihydrochloride (S)-P071	Histamine Receptor	Inflammation/Immunology
(S)-Cetirizine dihydrochloride ((S)-P071) is an orally active antagonist of the **histamine H1 receptor with a K_i** value of 39.1 nM. (S)-Cetirizine dihydrochloride exerts anti-allergic activity by binding to the histamine H1 receptor and blocking the action of histamine. (S)-Cetirizine dihydrochloride is promising for research of allergic diseases such as allergic rhinitis .

HY-107554

Methimepip dihydrobromide	Histamine Receptor	Neurological Disease
Methimepip dihydrobromide is a potent and selective **histamine H3 receptor agonist with an EC₅₀** of 0.316nM .

HY-19580

Ramixotidine CM 57755A	Histamine Receptor	Endocrinology
Ramisotidine is a **histamine H₂ receptor** antagonist that can inhibit gastric acid secretion stimulated by pentagastrin .

HY-124626

(R)-(+)-Mequitazine	Histamine Receptor	Inflammation/Immunology
(R)-(+)-Mequitazine is a **histamine H1 receptor** antagonist that mainly undergoes bio-transformation via human liver microsomes, resulting in hydroxylated and S-oxidized metabolites. (R)-(+)-Mequitazine competitively binds to the H1 receptors in gastrointestinal, vascular, and respiratory effect cells, thus blocking the endogenous activity of histamine. (R)-(+)-Mequitazine has an inhibitory effect on CYP3A-catalyzed midazolam 1’-hydroxylase. (R)-(+)-Mequitazine can be used in the study of various allergic diseases .

HY-108977

VUF 8430	Histamine Receptor	Neurological Disease
VUF 8430 is a potent and selective **histamine H4 receptor agonist with a K_i of 31.6 nM and an EC₅₀** of 50 nM .

HY-121455

Lamtidine	Histamine Receptor	Metabolic Disease
Lamtidine is a **histamine H₂ receptor** antagonist. Lamtidine has analogues and derivatives that exhibit stronger activity .

HY-30234S

Clemizole-d4	Histamine Receptor HCV TRP Channel	Cancer
Clemizole-d4 is a deuterium labeled Clemizole. Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication .

HY-19010

BMY-25368 SKF 94482	Histamine Receptor	Neurological Disease
BMY-25368 (SKF 94482) is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 competitively antagonizes gastric secretion stimulated by histamine and also antagonizes gastric secretion stimulated by Pentagastrin (HY-A0261), Bethanechol (HY-B0406), and food .

HY-15541

Zaltidine CP-57361	Histamine Receptor	Endocrinology
Zaltidine dihydrochloride (CP-5736 dihydrochloride) is a highly specific H2 receptor antagonist with antisecretion activity. Zaltidine dihydrochloride reduces the stimulant effect of histamine on gastric acid secretion by binding to histamine H2 receptors on gastric parietal cells, thus reducing gastric acid production. Zaltidine dihydrochloride can be used in the study of gastric acid-related diseases such as duodenal ulcers .

HY-15541A

Zaltidine dihydrochloride CP-5736 dihydrochloride	Histamine Receptor	Endocrinology
Zaltidine (CP-5736) dihydrochloride is a highly specific H2 receptor antagonist with antisecretion activity. Zaltidine dihydrochloride reduces the stimulant effect of histamine on gastric acid secretion by binding to histamine H2 receptors on gastric parietal cells, thus reducing gastric acid production. Zaltidine dihydrochloride can be used in the study of gastric acid-related diseases such as duodenal ulcers .

HY-119203

NNC 38-1049	Histamine Receptor	Metabolic Disease
NNC 38-1049 is an orally active, potent and competitive **histamine H3 receptor** antagonist. NNC 38-1049 produced an increase in extracellular levels of histamine in the paraventricular nucleus. NNC 38-1049 decreases food intake and body weight, which is promising for research of obesity .

HY-12200

GSK189254A hydrochloride GSK189254	Histamine Receptor	Neurological Disease
GSK189254A hydrochloride is a novel, potent and selective histamine H3 receptor antagonist with pK_i values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively .

HY-120531

UR-PI376	Histamine Receptor	Neurological Disease
UR-PI376 is a potent and selective histamine H4 receptor (H4R) agonist with a pEC₅₀ value of 7.47. UR-PI376 shows negligible hH1R and hH2R activities and moderate inverse agonistic activity at the hH3R .

HY-116560

ONO-8809	Histamine Receptor	Inflammation/Immunology
ONO-8809 is a Thromboxane A2 receptor antagonist. ONO-8809 inhibits the LTC4-induced airway hyperresponsiveness to histamine in a dose-dependent manner .

Cat. No.	Product Name

HY-L086

Neurodegenerative Disease-related Compound Library

3,545 compounds

Neurodegenerative diseases are incurable and life-threatening conditions that result in progressive degeneration and/or death of nerve cells. Some common neurodegenerative diseases include Alzheimer’s Disease (AD), Parkinson’s Disease (PD), Motor Neuron Disease (MND), Huntington’s Disease (HD), Spino-Cerebellar Ataxia (SCA), Spinal Muscular Atrophy (SMA), and Amyotrophic Lateral Sclerosis (ALS). Because the pathophysiology of neurodegenerative disorders is generally poorly understood, it is difficult to identify promising molecular targets and validate them. At the same time, about 85% of the drugs fail in clinical trials. Therefore, validating new targets and discovering new drugs to mitigate neurodegenerative disorders is need of the hour.

MCE offers a unique collection of 3,545 compounds with anti-Neurodegenerative Diseases activities or targeting the unique targets of neurodegenerative diseases. MCE Neurodegenerative Disease-related Compound Library is a useful tool for exploring the mechanism of neurodegenerative diseases and discovering new drugs for neurodegenerative diseases.

HY-L013

Neuronal Signaling Compound Library

3,802 compounds

Neuronal Signaling is involved in the regulation of the mechanisms of the central nervous system (CNS) such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of neurons and glia, neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells). G protein-coupled receptors (GPCRs), including 5-HT receptor, histamine receptor, opioid receptor, etc. are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation. GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as stroke, Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders.

MCE designs a unique collection of 3,802 Neuronal Signaling-related compounds that act as a useful tool for the research of neuronal regulation and neuronal diseases.

Cat. No.	Product Name	Type

HY-78924

N-Boc-D-prolinol	Biochemical Assay Reagents
N-Boc-D-prolinol is a protected chiral proline derivative. N-Boc-D-prolinol facilitates the synthesis of highly selective histamine H₁ and H₃ receptor antagonists. N-Boc-D-prolinol can be used in the research of allergic rhinitis .

HY-B0377G

Famotidine (GMP) MK-208 (GMP)	Biochemical Assay Reagents
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine GMP is a competitive histamine H2-receptor antagonist, inhibits gastric secretion, activates the gastric mucosal defensive mechanisms. Famotidine GMP ameliorates peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD) in rats model .

HY-W127737

Methylcobalamin hydrate

Mecobalamin hydrate

Biochemical Assay Reagents

Methylcobalamin Hydrate is a coenzyme required for methionine biosynthesis. Vitamins (hematopoiesis). It acts as a histamine receptor, Alzheimer study. Methylcobalamin is also used in the research of peripheral neuropathy, diabetic neuropathy, and as an initial research for amyotrophic lateral sclerosis. It can be used to prevent or research pathologies caused by vitamin B12 deficiency, such as pernicious anemia.

Cat. No.	Product Name	Target	Research Area

HY-P1237

C-Type Natriuretic Peptide (CNP) (1-22), human 2 Publications Verification	Histamine Receptor	Cardiovascular Disease Neurological Disease Metabolic Disease
C-Type Natriuretic Peptide (CNP) (1-22), human, a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor .

HY-P1237A

C-Type Natriuretic Peptide (CNP) (1-22), human TFA 2 Publications Verification	Histamine Receptor Endothelin Receptor	Cardiovascular Disease Neurological Disease Metabolic Disease
C-Type Natriuretic Peptide (CNP) (1-22), human (TFA),a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human (TFA) inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor .

HY-P2537

Apelin-12 2 Publications Verification	HIV Apelin Receptor (APJ)	Others
Apelin-12 is one of the most potent C-terminal fragments of the polypeptide that possesses a high affinity to orphan receptor APJ receptor. Apelin-12 is involved in the regulation of body fluid homeostasis and in the central control of feeding. Apelin-12 blocks HIV-1 entry through APJ receptor. Apelin-12 exerts neuroprotective effect .

HY-P10619

[Tyr6,D-Phe7,D-His9]-Substance P (6-11)	Neurokinin Receptor	Inflammation/Immunology
[Tyr6,D-Phe7,D-His9]-Substance P (6-11) is a tachykinin NK1 receptor antagonist that antagonizes Histamine (HY-B1204) induced hyperalgesia .

HY-P3317

Azaline Azaline A	GnRH Receptor	Endocrinology
Azaline (Azaline A) is a gonadotropin-releasing hormone (GnRH) receptor antagonist with a K_D value of 0.48 nM. Azaline can effectively induce histamine release, with an effect comparable to that of GnRH, and it can completely inhibit ovulation at a dose of 2.0-3.0 μg per female rat. Azaline has potential applications in regulating reproductive functions .

HY-P5357

SFNGGP-NH2	Protease Activated Receptor (PAR)	Others
SFNGGP-NH2 is a biological active peptide. (PAR-3 is a high-affinity thrombin receptor. PAR-3 mRNA is expressed in the cutaneous mast cells of humans. Protease-Activated Receptors (PARs) have been studied for their roles in itch and their itch-associated response through histamine-dependent/independent pathways have been reported. PAR-3 has been shown not to induce itching alone but possibly in conjunction with PAR-4. Co-expression of PAR-3 and PAR-4 enhances thrombin action suggesting that PAR-3 alone does not mediate transmembrane signaling but instead functions as a cofactor to activate PAR-4.)

HY-P11411

[D-Tyr27,36, D-Thr32]-Neuropeptide Y (27-36), rat	Neuropeptide Y Receptor Histamine Receptor	Cardiovascular Disease
[D-Tyr27,36, D-Thr32]-Neuropeptide Y (27-36), rat is a fragment analogue of a neuropeptide Y (NPY) with cardiovascular activity. [D-Tyr27,36, D-Thr32]-Neuropeptide Y (27-36), rat can induce profound and sustained hypotension in both hypertensive and normotensive rats and its antihypertensive effect is partly attributed to its activity on **histamine receptor**. [D-Tyr27,36, D-Thr32]-Neuropeptide Y (27-36), rat can be used for studying antihypertensive effects .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B1204

Histamine Maximum Cited Publications 20 Publications Verification Ergamine	Structural Classification Natural Products Human Gut Microbiota Metabolites Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Endocrinology Cancer	Histamine Receptor p38 MAPK Akt Reactive Oxygen Species (ROS) Apoptosis Endogenous Metabolite
Histamine is the agonist for **histamine receptor** and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-17042

Cetirizine 3 Publications Verification	Classification of Application Fields Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Endocrinology Source Classification	Histamine Receptor
Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine *H1-receptor* antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .

HY-B0539

Desloratadine 10+ Cited Publications Sch34117	Structural Classification Natural Products Classification of Application Fields Endogenous metabolite Disease Research Fields Endocrinology	Histamine Receptor TNF Receptor Leukotriene Receptor
Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (K_i=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria .

HY-B0303

Diphenhydramine 5+ Cited Publications	Alkaloids Classification of Application Fields Other Alkaloids Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Histamine Receptor Bacterial Endogenous Metabolite iGluR
Diphenhydramine is a first-generation **histamine H1-receptor** antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .

HY-B0722

Histamine dihydrochloride Maximum Cited Publications 20 Publications Verification	Structural Classification Natural Products Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Histamine Receptor p38 MAPK Akt Reactive Oxygen Species (ROS) Apoptosis Endogenous Metabolite
Histamine dihydrochloride is the agonist for **histamine receptor** and a vasodilator. Histamine dihydrochloride is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine dihydrochloride affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-B0303A

Diphenhydramine hydrochloride 5+ Cited Publications	Alkaloids Classification of Application Fields Other Alkaloids Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Histamine Receptor Endogenous Metabolite Bacterial Apoptosis
Diphenhydramine hydrochloride is a first-generation **histamine H1-receptor** antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .

HY-A0129

Histamine phosphate Maximum Cited Publications 20 Publications Verification Histamine diphosphate	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Endocrinology Source Classification Cancer	Histamine Receptor p38 MAPK Akt Reactive Oxygen Species (ROS) Apoptosis Endogenous Metabolite
Histamine phosphate is the agonist for **histamine receptor** and a vasodilator. Histamine phosphate is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine phosphate affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine phosphate can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-N0054

Osthole 15+ Cited Publications Osthol; NSC 31868	Cardiovascular Disease Classification of Application Fields Coumarins Plants Biological Pesticide Research Agricultural Research Infection other families Phenylpropanoids Inflammation/Immunology Disease Research Fields Endocrinology Source Classification	Histamine Receptor Apoptosis Parasite HBV
Osthole (Osthol) is a natural antihistamine alternative. Osthole may be a potential inhibitor of **histamine H₁ receptor activity. Osthole also suppresses the secretion of HBV** in cells.

HY-B0157

Ketotifen 3 Publications Verification HC 20-511	Infection Natural Products Classification of Application Fields Endogenous metabolite Inflammation/Immunology Disease Research Fields Endocrinology Source Classification	Endogenous Metabolite Histamine Receptor SARS-CoV Influenza Virus
Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention .

HY-B0157A

Ketotifen fumarate 3 Publications Verification HC 20511 fumarate	Natural Products Classification of Application Fields Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Histamine Receptor Endogenous Metabolite SARS-CoV Influenza Virus
Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen fumarate also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention .

HY-113413

Imidazoleacetic acid 2 Publications Verification Imidazolyl-4-acetic acid	Structural Classification Human Gut Microbiota Metabolites Classification of Application Fields Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite GABA Receptor
Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABA_A receptor. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity .

HY-A0191

Dexbrompheniramine (+)-Brompheniramine; (S)-Brompheniramine	Structural Classification Natural Products Classification of Application Fields Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Endogenous Metabolite Histamine Receptor TRP Channel
Dexbrompheniramine ((+)-Brompheniramine; (S)-Brompheniramine) is a dual inhibitor of **histamine H1 receptor and TRPV1** receptor that can cross the blood-brain barrier. Dexbrompheniramine exerts its effects by functionally blocking H1 receptor activity and dose-dependently inhibiting TRPV1-mediated calcium responses, including Capsaicin (HY-10448)-induced responses. The combination of Dexbrompheniramine with Cimetidine (HY-14289) eliminates histamine-induced and sham-feeding-induced drinking behavior, whereas Dexbrompheniramine alone does not induce thirst or alter sham-feeding behavior in rats. Dexbrompheniramine can be used in the research of chronic cough and related pathological mechanisms .

HY-107566

Conessine	Infection other families Classification of Application Fields Plants Disease Research Fields Steroids Source Classification	Histamine Receptor Parasite MDM-2/p53 NF-κB FOXO Bacterial
Conessine is an orally active and BBB-penetrable selective **histamine H3 receptor antagonist. The pK_i** values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy .

HY-B0426A

Olopatadine hydrochloride ALO4943A; KW4679	Structural Classification Alkaloids Classification of Application Fields Ketones, Aldehydes, Acids Other Alkaloids Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Histamine Receptor CXCR
Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active **histamine H1 receptor** antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4 ⁺ and CD8 ⁺ T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis .

HY-17428

Tripelennamine hydrochloride	Structural Classification Alkaloids Classification of Application Fields Pyridine Alkaloids Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Histamine Receptor
Tripelennamine hydrochloride is a histamine H1-receptor antagonist. Tripelennamine hydrochloride effectively reverses histamine-induced bronchoconstriction, increased transpulmonary pressure, elevated pulmonary vascular resistance and reduced dynamic compliance. Tripelennamine hydrochloride does not significantly affect arterial hypoxemia, hemoglobin desaturation and hypercapnia in horses undergoing short-term high-intensity exercise. Tripelennamine hydrochloride exhibits local and central analgesic activity. Tripelennamine hydrochloride can be used in studies related to emphysema, urticaria and acute laminitis .

HY-A0027

Fenspiride hydrochloride	Classification of Application Fields Disease Research Fields Endocrinology	Histamine Receptor Phosphodiesterase (PDE)
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC₅₀ values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .

HY-N0742

Absinthin	Triterpenes Classification of Application Fields Terpenoids Other Diseases Plants Acacia confusa Merr. Compositae Disease Research Fields Source Classification	Others
Absinthin is a structurally unique triterpene, and is responsible for the high bitter value of wormwood. Absinthin is an agonist of the bitter taste receptor hTAS2R46, which reduces cytosolic Ca ²⁺-rises induced by histamine by a receptor-specific mechanism mediated by hTAS2R46 .

HY-W062109

Olopatadine	Structural Classification Alkaloids Classification of Application Fields Other Alkaloids Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Histamine Receptor CXCR
Olopatadine (ALO4943A; KW4679) is an orally active **histamine H1 receptor** antagonist and mast cell stabilizer. Olopatadine exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine also reduces the expression levels of CXCR3 on the surface of CD4 ⁺ and CD8 ⁺ T cells. Olopatadine inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis .

HY-B1204R

Histamine (Standard) Ergamine (Standard)	Structural Classification Natural Products Human Gut Microbiota Metabolites Microorganisms Endogenous metabolite	Reference Standards Histamine Receptor p38 MAPK Akt Reactive Oxygen Species (ROS) Apoptosis Endogenous Metabolite
Histamine (Standard) is the analytical standard of Histamine (HY-B1204). This product is intended for research and analytical applications. Histamine is the agonist for **histamine receptor** and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-B0722R

Histamine dihydrochloride (Standard)	Structural Classification Natural Products Endogenous metabolite Source Classification	Reference Standards Histamine Receptor p38 MAPK Akt Reactive Oxygen Species (ROS) Apoptosis Endogenous Metabolite
Histamine dihydrochloride (Standard) is the analytical standard of Histamine dihydrochloride (HY-B0722). This product is intended for research and analytical applications. Histamine dihydrochloride is the agonist for **histamine receptor** and a vasodilator. Histamine dihydrochloride is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine dihydrochloride affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-B0303R

Diphenhydramine (Standard)	Structural Classification Alkaloids Other Alkaloids Endogenous metabolite Source Classification	Reference Standards Histamine Receptor Bacterial Endogenous Metabolite iGluR
Diphenhydramine (Standard) is the analytical standard of Diphenhydramine. This product is intended for research and analytical applications. Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .

HY-A0178

Isothipendyl AY 56012	Alkaloids Classification of Application Fields Pyridine Alkaloids Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Histamine Receptor Endogenous Metabolite
Isothipendyl (AY 56012), an azaphenothiazine derivative, is a potent histamine 1 (H1) receptor antagonist. Isothipendyl is a primary metabolite .

HY-B0426AR

Olopatadine hydrochloride (Standard) ALO4943A (Standard); KW4679 (Standard)	Structural Classification Alkaloids Ketones, Aldehydes, Acids Other Alkaloids Endogenous metabolite Source Classification	Reference Standards Histamine Receptor CXCR
Olopatadine (hydrochloride) (Standard) is the analytical standard of Olopatadine (hydrochloride). This product is intended for research and analytical applications. Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active **histamine H1 receptor** antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4 ⁺ and CD8 ⁺ T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis .

HY-B0157AR

Ketotifen fumarate (Standard) HC 20511 fumarate (Standard)	Structural Classification Natural Products Endogenous metabolite Source Classification	Reference Standards Histamine Receptor Endogenous Metabolite SARS-CoV Influenza Virus
Ketotifen (fumarate) (Standard) is the analytical standard of Ketotifen (fumarate). This product is intended for research and analytical applications. Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen fumarate also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention .

HY-117500

Aplysamine-1	Alkaloids Animals Other Alkaloids Marine natural products Sponge Source Classification	Histamine Receptor
Aplysamine-1 acts as an antagonist for the histamine H3 receptor.

HY-A0129R

Histamine phosphate (Standard) Histamine diphosphate (Standard)	Alkaloids Structural Classification Other Alkaloids Endogenous metabolite Source Classification	Reference Standards Histamine Receptor p38 MAPK Akt Reactive Oxygen Species (ROS) Apoptosis Endogenous Metabolite
Histamine phosphate (Standard) is the analytical standard of Histamine phosphate (HY-A0129). This product is intended for research and analytical applications. Histamine phosphate is the agonist for **histamine receptor** and a vasodilator. Histamine phosphate is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine phosphate affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine phosphate can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-17428A

Tripelennamine	Structural Classification Alkaloids Classification of Application Fields Pyridine Alkaloids Endogenous metabolite Inflammation/Immunology Disease Research Fields Endocrinology Source Classification	Histamine Receptor
Tripelennamine is a histamine H1-receptor antagonist. Tripelennamine effectively reverses histamine-induced bronchoconstriction, increased transpulmonary pressure, elevated pulmonary vascular resistance and reduced dynamic compliance. Tripelennamine does not significantly affect arterial hypoxemia, hemoglobin desaturation and hypercapnia in horses undergoing short-term high-intensity exercise. Tripelennamine exhibits local and central analgesic activity. Tripelennamine can be used in studies related to emphysema, urticaria and acute laminitis .

HY-17428B

Tripelennamine citrate	Structural Classification Alkaloids Classification of Application Fields Pyridine Alkaloids Endogenous metabolite Inflammation/Immunology Disease Research Fields Endocrinology Source Classification	Histamine Receptor
Tripelennamine citrate is a histamine H1-receptor antagonist. Tripelennamine citrate effectively reverses histamine-induced bronchoconstriction, increased transpulmonary pressure, elevated pulmonary vascular resistance and reduced dynamic compliance. Tripelennamine citrate does not significantly affect arterial hypoxemia, hemoglobin desaturation and hypercapnia in horses undergoing short-term high-intensity exercise. Tripelennamine citrate exhibits local and central analgesic activity. Tripelennamine citrate can be used in studies related to emphysema, urticaria and acute laminitis .

HY-17428R

Tripelennamine hydrochloride (Standard)	Structural Classification Alkaloids Pyridine Alkaloids Endogenous metabolite Source Classification	Reference Standards Histamine Receptor
Tripelennamine hydrochloride (Standard) is the analytical standard of Tripelennamine hydrochloride (HY-17428). This product is intended for research and analytical applications. Tripelennamine hydrochloride is a histamine H1-receptor antagonist. Tripelennamine hydrochloride effectively reverses histamine-induced bronchoconstriction, increased transpulmonary pressure, elevated pulmonary vascular resistance and reduced dynamic compliance. Tripelennamine hydrochloride does not significantly affect arterial hypoxemia, hemoglobin desaturation and hypercapnia in horses undergoing short-term high-intensity exercise. Tripelennamine hydrochloride exhibits local and central analgesic activity. Tripelennamine hydrochloride can be used in studies related to emphysema, urticaria and acute laminitis .

HY-N0054R

Osthole (Standard) Osthol (Standard); NSC 31868 (Standard)	Structural Classification other families Coumarins Phenylpropanoids Plants Source Classification	Reference Standards Histamine Receptor Apoptosis Parasite HBV
Osthole (Standard) is the analytical standard of Osthole. This product is intended for research and analytical applications. Osthole (Osthol) is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity. Osthole also suppresses the secretion of HBV in cells.

HY-17042R

Cetirizine (Standard)	Structural Classification Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards Histamine Receptor
Cetirizine (Standard) is the analytical standard of Cetirizine. This product is intended for research and analytical applications. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine *H1-receptor* antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .

HY-N1514R

Ganoderenic acid B (Standard)	Triterpenes Structural Classification Human Gut Microbiota Metabolites Microorganisms Terpenoids Polyporaceae Ganoderma lucidum (Leyss. Ex Fr.) Karst. Plants Endogenous metabolite Source Classification	Reference Standards P-glycoprotein
Doxylamine (succinate) (Standard) is the analytical standard of Doxylamine (succinate). This product is intended for research and analytical applications. Doxylamine (succinate), a first generation antihistamine, is a histamine (H1) receptor antagonist. Doxylamine is also a local analgesic agent and effective hypnotic agent .

HY-N7814R

2-Hydroxypalmitic acid (Standard)	Structural Classification Microorganisms Ketones, Aldehydes, Acids Source Classification	Reference Standards Endogenous Metabolite
Pheniramine (maleate) (Standard) is the analytical standard of Pheniramine (maleate). This product is intended for research and analytical applications. Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .

HY-113413R

Imidazoleacetic acid (Standard) Imidazolyl-4-acetic acid (Standard)	Structural Classification Human Gut Microbiota Metabolites Microorganisms Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite GABA Receptor
Imidazoleacetic acid (Standard) is the analytical standard of Imidazoleacetic acid (HY-113413). This product is intended for research and analytical applications. Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABA_A receptor. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity .

HY-B0157R

Ketotifen (Standard) HC 20-511 (Standard)	Structural Classification Natural Products Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite Histamine Receptor SARS-CoV Influenza Virus
Ketotifen (Standard) is the analytical standard of Ketotifen. This product is intended for research and analytical applications. Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention .

HY-N0742R

Absinthin (Standard)	Triterpenes Structural Classification Terpenoids Plants Acacia confusa Merr. Compositae Source Classification	Reference Standards Others
Absinthin (Standard) is the analytical standard of Absinthin. This product is intended for research and analytical applications. Absinthin is a structurally unique triterpene, and is responsible for the high bitter value of wormwood. Absinthin is an agonist of the bitter taste receptor hTAS2R46, which reduces cytosolic Ca2+-rises induced by histamine by a receptor-specific mechanism mediated by hTAS2R46 .

HY-N11725

Phlorofucofuroeckol A	Structural Classification Microorganisms Phenols Polyphenols Source Classification	Fc Receptor (FcR)
Phlorofucofuroeckol A is a FcεRI inhibitor with low cytotoxicity toward basophilic leukemia cells. Phlorofucofuroeckol A suppresses binding activity between IgE and FcεRI receptor. Phlorofucofuroeckol A inhibits histamine release from basophilic leukemia cells stimulated by IgE/anti-IgE or calcium ionophore A23187 (HY-N6687). Phlorofucofuroeckol A inhibits β-hexosaminidase release from basophilic leukemia cells stimulated by IgE/DNP-BSA. Phlorofucofuroeckol A can be used for the research of allergy disease .

Recombinant Proteins Recommended:

Histamine Receptor

Species:	Human (3)
Tag:	GFP (1) His (2)
Source:	HEK293 (2) E. coli (1)

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P702323

	HRH3-VLPs Protein, Human (HEK293, His) Histamine H3 receptor; G-protein coupled receptor 97	Human	HEK293
	HRH3-VLPs Protein, Human (HEK293, His) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P701236. Tags can only be detected under denaturing conditions.

HY-P702322

	HRH3-VLPs Protein, Human (HEK293, GFP) Histamine H3 receptor; G-protein coupled receptor 97	Human	HEK293
	HRH3-VLPs Protein, Human (HEK293, GFP) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P701236. Tags can only be detected under denaturing conditions.

HY-P702580

	HRH1 Protein, Human (His) Histamine H1 receptor; H1R; HH1R	Human	E. coli
	HRH1 Protein, Human (His) is the recombinant human-derived HRH1, expressed by E. coli , with N-6*His labeled tag.

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Cat. No.	Product Name	Chemical Structure

HY-B0303AS

Diphenhydramine-d6 hydrochloride
Diphenhydramine-d₆ (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .

HY-17043S1

Loratadine-d5
Loratadine-d₅ is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.

HY-B0303AS1

Diphenhydramine-d5 hydrochloride
Diphenhydramine-d₅ (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .

HY-17042S1

Cetirizine-d8
Cetirizine-d₈ is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .

HY-B1204S1

Histamine-d4

Histamine-d₄ (Ergamine-d₄) is deuterium labeled Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-A0077S1

Perphenazine-d4
Perphenazine-d₄ is the deuterium labeled Perphenazine. Perphenazine is a typical antipsychotic agent, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.

HY-B0814S1

Levocetirizine-d4

Levocetirizine-d₄ ((R)-Cetirizine-d₄) is the deuterium-labeled Levocetirizine (HY-B0814) . Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .

HY-W062109S

Olopatadine-d6

Olopatadine-d₆ is the deuterium labeled Olopatadine. Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4 ⁺ and CD8 ⁺ T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis .

HY-12532S

Astemizole-d3
Astemizole-d₃ is the deuterium labeled Astemizole. Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole has antipruritic effects .

HY-B0725S

Doxepin-d3 hydrochloride
Doxepin-d₃ (hydrochloride) is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2 .

HY-B0548S1

Hydroxyzine D8
Hydroxyzine-d₈ is deuterium labeled Hydroxyzine. Hydroxyzine is a histamine H1-receptor antagonist .

HY-B1204S2

Histamine-13C5, 15N3

Histamine- ¹³C₅, ¹⁵N₃ (Ergamine- ¹³C₅, ¹⁵N₃) is the ¹³C and ¹⁵N labeled isotope of Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-B1296S

Promethazine-d6 hydrochloride
Promethazine-d₆ (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is an orally active histamine receptor antagonist .

HY-B1895S

Levodropropizine-d8
Levodropropizine-d₈ is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is a histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.

HY-B0377S

Famotidine-13C,d3
Famotidine- ¹³C,d₃ is the ¹³C- and deuterium labeled Famotidine. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.

HY-W707517

Famotidine-d4
Famotidine-d₄ (MK-208-d₄) is deuterium labeled Famotidine. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion .

HY-B0548AS1

Hydroxyzine-d4' dihydrochloride
Hydroxyzine-d₄ (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .

HY-17042S

Cetirizine-d4
Cetirizine-d₄ is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].

HY-B0426AS

Olopatadine-d3 hydrochloride

Olopatadine-d₃ hydrochloride (ALO4943A-d₃) is the deuterium labeled Olopatadine hydrochloride. Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4 ⁺ and CD8 ⁺ T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis .

HY-B0310S

Nizatidine-d3
Nizatidine-d₃ is the deuterium labeled Nizatidine. Nizatidine is a potent and orally active histamine H2 receptor antagonist, can be used for the research of stomach?and?intestines ulcers. Nizatidine works by decreasing the secretion of gastric?acid the stomach makes and prevent ulcers from coming back after they have healed in animal models .

HY-B0640S

Epinastine-13C,d3 hydrobromide
Epinastine- ¹³C,d₃ (hydrobromide) is the ¹³C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action .

HY-B0352S3

Mirtazapine-d4 hydrochloride
Mirtazapine-d₄ hydrochloride is deuterated labeled Mirtazapine (HY-B0352). Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT₂, 5-HT₃, **histamine H1 receptor and α2-adrenoceptor antagonist with pK_i** values of 8.05, 8.1, 9.3 and 6.95, respectively .

HY-B2169S2

Melperone-d4 hydrochloride

Melperone-d₄ hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) . Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .

HY-B1510S

Acrivastine D7
Acrivastine-d₇ is a deuterium labeled Acrivastine. Acrivastine is a short acting histamine 1 receptor antagonist.

HY-30234S

Clemizole-d4
Clemizole-d4 is a deuterium labeled Clemizole. Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication .

HY-10121S2

Asenapine-13C,d3
Asenapine- ¹³C,d₃ is ¹³C and deuterated labeled Asenapine (HY-10121). Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and **histamine receptors (pK_i**: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder .

HY-W769200

Asenapine-13C,d3 maleate

Asenapine- ¹³C,d₃ Maleate is the deuterium labeled and ¹³C-Asenapine Maleate (HY-11100). Asenapine (Org 5222) Maleate, an atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and histamine receptors (pK_i: 8.2-9.0). Asenapine Maleate can be used in the research of schizophrenia and bipolar disorder .

HY-B1204S4

Histamine-15N3

Histamine- ¹⁵N₃ is the ¹⁵N₃-labeled Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-B1589AS

Carbinoxamine-d6 maleate
Carbinoxamine-d₆ (maleate) is the deuterium labeled Carbinoxamine maleate salt. Carbinoxamine maleate salt is a histamine H1 receptor antagonist.

HY-B0281AS

Ranitidine-d6 hydrochloride

Ranitidine-d₆ hydrochloride is the deuterium labeled Ranitidine hydrochloride (HY-B0281A) . Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA₂ values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice .

HY-B0693S

Ranitidine-d6

Ranitidine-d₆ is the deuterium labeled Ranitidine (HY-B0693). Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice .

HY-B0548AS

Hydroxyzine-d4 dihydrochloride
Hydroxyzine-d₄ (dihydrochloride) is deuterium labeled Hydroxyzine. Hydroxyzine is a heterocyclic histamine H1-receptor antagonist. Hydroxyzine has anticholinergic, anxiolytic and analgesic properties .

HY-19489S1

(Rac)-Levomepromazine-d3 hydrochloride
(Rac)-Levomepromazine-d₃ (hydrochloride) is a labelled racemic Methotrimeprazine, which is a phenothiazine which has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors .

HY-A0077S2

Perphenazine-d6 fumarate

Perphenazine-d6 (fumarate) is a deuterated labeled Perphenazine . Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with K_i values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation .

HY-B0524AS

Betahistine-d3 dihydrochloride
Betahistine-d₃ (dihydrochloride) is the deuterium labeled Betahistine dihydrochloride. Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA) .

HY-14447S

Bilastine-d6
Bilastine-d₆ is the deuterium labeled Bilastine. Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria .

HY-B0377S1

Famotidine-13C
Famotidine- ¹³C (MK-208- ¹³C) is ¹³C labeled Famotidine. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.

HY-B0524AS1

Betahistine-13C,d3 dihydrochloride
Betahistine- ¹³C,d₃ (dihydrochloride) is the ¹³C- and deuterium labeled Betahistine (dihydrochloride). Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA) .

HY-B0298AS

Clemastine-d5 fumarate

1 Publications Verification

Clemastine (HS-592; Meclastine)-d₅ fumarate is the deuterium labeled Clemastine fumarate. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .

HY-B0160S

Lafutidine-d10
Lafutidine-d₁₀ is deuterium labeled Lafutidine. Lafutidine (FRG-8813) is a histamine H2-receptor antagonist (H2RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease .

HY-B0349S

Meclizine-d8
Meclizine-d₈ is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .

HY-B0548AS2

Hydroxyzine-d8 dihydrochloride
Hydroxyzine-d₈ (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .

HY-B0274AS

Chlorprothixene-d6 hydrochloride
Chlorprothixene-d₆ hydrochloride is the deuterium labeled Chlorprothixene hydrochloride. Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with K_is of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity .

HY-B0814S

Levocetirizine-d4 dihydrochloride

Levocetirizine-d₄ (dihydrochloride) is the deuterium labeled Levocetirizine. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].

HY-12199S1

Pitolisant-d6
Pitolisant-d₆ (Tiprolisant-d₆) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human **histamine H3 receptor (K_i**=0.16 nM).

HY-17043S

Loratadine-d4
Loratadine-d₄ is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.

HY-14447S1

Bilastine-d4
Bilastine-d₄ is deuterium labeled Bilastine. Bilastine is an oral **histamine H1-receptor** antagonist. Bilastine can be used for allergic rhinitis and urticaria studies, and it also improves diabetic nephropathy in mice, showing safety for the central nervous system .

HY-W777002

Famotidine-13C3
Famotidine- ¹³C₃ (MK-208- ¹³C₃) is the ¹³C-labeled Famotidine (HY-B0377). Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.

HY-B1397S

Cyclizine-d3
Cyclizine-d₃ is deuterium labeled Cyclizine. Cyclizine, a piperazine-derivative, is a potent and selective **histamine H1 receptor** antagonist. Cyclizine can be used for the research of nausea, vomiting, and dizziness .

HY-12199S

Pitolisant-d10
Pitolisant-d₁₀ (Tiprolisant-d₁₀) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human **histamine H3 receptor (K_i**=0.16 nM) .

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HY-P82956

	HRH3 Antibody (YA2701) HRH3; GPCR97; Histamine H3 receptor; H3R; HH3R; G-protein coupled receptor 97	WB, ICC/IF, FC	Human, Mouse, Rat
	HRH3 Antibody (YA2701) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to HRH3.

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HY-105535

Etintidine hydrochloride BL-5641 hydrochloride		Alkynes
Etintidine (BL-5641) hydrochloride is a potent orally active **histamine H2-receptor** antagonist. Etintidine hydrochloride can be used for gastrointestinal ulcer diseases research .

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