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Results for "

human H1 receptors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (5) Adrenergic Receptor (2) Amyloid-β (1) Apoptosis (6) Calcium Channel (1) CCR (1) CDK (1) Checkpoint Kinase (Chk) (1) Cytochrome P450 (1) Dopamine Receptor (1) Drug Derivative (2) Histamine Receptor (18) iGluR (1) Isotope-Labeled Compounds (1) Leukotriene Receptor (1) mAChR (1) nAChR (1) p38 MAPK (1) PARP (1) Potassium Channel (1) Reference Standards (2) SARS-CoV (1) TNF Receptor (1)
By Research Areas:	Cancer (4) Endocrinology (3) Inflammation/Immunology (12) Metabolic Disease (3) Neurological Disease (9)

By Targets:

5-HT Receptor (5)

Adrenergic Receptor (2)

Amyloid-β (1)

Apoptosis (6)

Calcium Channel (1)

CCR (1)

CDK (1)

Checkpoint Kinase (Chk) (1)

Cytochrome P450 (1)

Dopamine Receptor (1)

Drug Derivative (2)

Histamine Receptor (18)

iGluR (1)

Isotope-Labeled Compounds (1)

Leukotriene Receptor (1)

mAChR (1)

nAChR (1)

p38 MAPK (1)

PARP (1)

Potassium Channel (1)

Reference Standards (2)

SARS-CoV (1)

TNF Receptor (1)

By Research Areas:

Cancer (4)

Endocrinology (3)

Inflammation/Immunology (12)

Metabolic Disease (3)

Neurological Disease (9)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0539

Desloratadine 10+ Cited Publications Sch34117	Histamine Receptor TNF Receptor Leukotriene Receptor	Inflammation/Immunology
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-B0349

Meclizine dihydrochloride 4 Publications Verification Meclozine dihydrochloride	Histamine Receptor Apoptosis	Neurological Disease Endocrinology Cancer
Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse *constitutive androstane receptor* (CAR)** and an inverse agonist for Human CAR .

HY-B1165

Cyproheptadine (hydrochloride sesquihydrate) 3 Publications Verification	p38 MAPK Checkpoint Kinase (Chk) Histamine Receptor 5-HT Receptor CDK PARP Apoptosis	Cancer
Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia .

HY-B0170A

Azatadine dimaleate Azatadine maleate	Histamine Receptor SARS-CoV	Inflammation/Immunology
Azatadine dimaleate (Azatadine maleate) is an orally active histamine H₁ receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine dimaleate induces sedation and exhibits topical anesthetic properties. Azatadine dimaleate can be used for the research of allergic rhinitis .

HY-148825

NP10679	iGluR Histamine Receptor Potassium Channel Cytochrome P450 Adrenergic Receptor	Metabolic Disease Inflammation/Immunology Cancer
NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC₅₀s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC₅₀s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes .

HY-106587A

Octoclothepin maleate salt Clorotepine maleate salt	Drug Derivative 5-HT Receptor	Neurological Disease
Octoclothepin (Clorotepine) maleate salt is a D₂ dopamine receptor antagonist and 5-HT₂ serotonin receptor antagonist , with K_i values of 0.67 nM, 0.57 nM, and 0.19 nM for the dopamine D₂, 5-HT_2A, and 5-HT_2C receptors, respectively. Octoclothepin maleate salt also binds to adrenergic receptors, with K_i values of 0.66 nM, 0.56 nM, and 0.77 nM for α_1a, α_1b, and α_1d, respectively. Octoclothepin maleate salt can be used in schizophrenia research .

HY-B0349A

Meclizine Meclozine	Histamine Receptor Apoptosis	Neurological Disease Inflammation/Immunology
Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse *constitutive androstane receptor* (CAR)** and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease .

HY-101601

Bamirastine TAK-427	Histamine Receptor	Inflammation/Immunology Endocrinology
Bamirastine inhibits ligand binding to recombinant human histamine H₁ receptors (rhH₁R) with an IC₅₀ value of 17.3 nM.

HY-B0170

Azatadine	Histamine Receptor mAChR nAChR 5-HT Receptor	Inflammation/Immunology
Azatadine is an orally active histamine H₁ receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine induces sedation and exhibits topical anesthetic properties. Azatadine can be used for the research of allergic rhinitis .

HY-B0349B

Meclizine dihydrochloride monohydrate Meclozine dihydrochloride monohydrate	Histamine Receptor Apoptosis	Neurological Disease Inflammation/Immunology
Meclizine (Meclozine) dihydrochloride monohydrate, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouse *constitutive androstane receptor* (CAR)** and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease .

HY-B0349R

Meclizine dihydrochloride (Standard) Meclozine dihydrochloride (Standard)	Reference Standards Histamine Receptor Apoptosis	Neurological Disease Endocrinology Cancer
Meclizine (dihydrochloride) (Standard) is the analytical standard of Meclizine (dihydrochloride). This product is intended for research and analytical applications. Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .

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-170789

H1R ligand-1	Histamine Receptor	Neurological Disease
H1R ligand-1 (Compound fragment 1) is a high-affinity ligand for the human histamine H1 receptor (H1R). H1R ligand-1 can be used as a scaffold to design and synthesize a set of derivatives to explore H1R binding kinetics .

HY-B0349S

Meclizine-d8 Meclozine-d₈	Isotope-Labeled Compounds Histamine Receptor Apoptosis	Inflammation/Immunology
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-14939A

Vapitadine hydrochloride	Histamine Receptor	Inflammation/Immunology
Vapitadine hydrochloride (Compound 3a) is a selective, orally active and nonsedating antihistamine agent, which exhibits a good binding affinity with human cloned histamine H1 receptor with a K_i of 19 nM. Vapitadine hydrochloride decreases the histamine-induced lethality (ED₅₀ is 0.056-1.2 mg/kg), antagonizes the cutaneous reactions to histamine (ED₅₀ is 0.51-1.4 mg/kg) in rats .

HY-167897

UR-AK49	Histamine Receptor	Neurological Disease
UR-AK49 (compound 11) is a human histamine H1 and H2 receptor agonist. UR-AK49 has an EC₅₀ of 23 nM in a GTPase assay with hH2R-Gsalpha fusion protein expressed in Sf9 insect cells. UR-AK49 can be used in neuro-related research .

HY-156049

MG-H1	Amyloid-β	Metabolic Disease
MG-H1 is a receptor of advanced glycation end products (RAGE) ligand with a K_d of 4.12 nM. MG-H1 can bind to human umbilical vein endothelial cell. MG-H1 can be used for research of diabetes .

HY-B0170AR

Azatadine dimaleate (Standard) Azatadine maleate (Standard)	Histamine Receptor Reference Standards	Metabolic Disease Inflammation/Immunology
Azatadine dimaleate (Standard) is the analytical standard of Azatadine dimaleate. This product is intended for research and analytical applications. Azatadine dimaleate (Azatadine maleate) is an orally active histamine H₁ receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine dimaleate induces sedation and exhibits topical anesthetic properties. Azatadine dimaleate can be used for the research of allergic rhinitis .

HY-106587

Octoclothepine Clorotepine	5-HT Receptor Drug Derivative	Neurological Disease
Octoclothepin (Clorotepine) is a D₂ dopamine receptor antagonist and 5-HT₂ serotonin receptor antagonist , with K_i values of 0.67 nM, 0.57 nM, and 0.19 nM for the dopamine D₂, 5-HT_2A, and 5-HT_2C receptors, respectively. Octoclothepin also binds to adrenergic receptors, with K_i values of 0.66 nM, 0.56 nM, and 0.77 nM for α_1a, α_1b, and α_1d, respectively. Octoclothepin can be used in schizophrenia research .

HY-106587B

Octoclothepin dimaleate Clorotepine dimaleate	Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease
Octoclothepin (Clorotepine) dimaleate is a D₂ dopamine receptor antagonist and 5-HT₂ serotonin receptor antagonist , with K_i values of 0.67 nM, 0.57 nM, and 0.19 nM for the dopamine D₂, 5-HT_2A, and 5-HT_2C receptors, respectively. Octoclothepin dimaleate also binds to adrenergic receptors, with K_i values of 0.66 nM, 0.56 nM, and 0.77 nM for α_1a, α_1b, and α_1d, respectively. Octoclothepin dimaleate can be used in schizophrenia research .

HY-124912

VUF-6884	Histamine Receptor	Others
VUF-6884 (Compound 7j) is a histamine receptor (Histamine Receptor) ligand with activity toward human H4R and *H1R. Its pEC₅₀* and pK_i values against human H4R are 7.70 and 7.55, respectively, while those against human *H1R* are 8.17 and 8.11, respectively. VUF-6884 competitively binds to the orthosteric binding site of human H4R to displace histamine, and exhibits inverse agonist activity at human *H1R* .

HY-182736

YM-344484	CCR Histamine Receptor Calcium Channel	Inflammation/Immunology
YM-344484 is an orally active dual antagonist of chemokine CCR3 receptor and histamine histamine H1 receptor. YM-344484 inhibits ligand-induced Ca ²⁺ influx, chemotaxis of CCR3-expressing cells, histamine-induced Ca ²⁺ influx, increased vascular permeability and eosinophil accumulation. YM-344484 suppresses vascular permeability and inhibits eosinophil infiltration in a mouse asthma model. YM-344484 can be used in research related to asthma, allergic rhinitis and atopic dermatitis .

Cat. No.	Product Name	Category	Target	Chemical Structure

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 .

Cat. No.	Product Name	Chemical Structure

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 .

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