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Isoforms Recommended:	H₁ Receptor

Results for "

H1+receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (23) Adrenergic Receptor (23) Akt (1) Amyloid-β (6) Antibiotic (1) Apoptosis (19) Autophagy (2) Bacterial (11) Calcium Channel (5) CCR (2) CDK (1) Checkpoint Kinase (Chk) (1) CXCR (6) Cytochrome P450 (5) Dengue Virus (4) Dopamine Receptor (13) Dopamine Transporter (4) Drug Derivative (1) Drug Intermediate (2) Drug Metabolite (8) Endogenous Metabolite (22) Environmental Pollutants (1) ERK (5) Flavivirus (4) HBV (4) Histamine Receptor (251) iGluR (2) Influenza Virus (8) Integrin (3) Interleukin Related (5) Isotope-Labeled Compounds (49) Leukotriene Receptor (1) Lipoxygenase (1) mAChR (16) Macrophage migration inhibitory factor (MIF) (1) mGluR (3) MOFs (1) Neurotensin Receptor (3) Opioid Receptor (5) P-glycoprotein (1) p38 MAPK (6) Parasite (3) PARP (1) Potassium Channel (14) Reference Standards (67) SARS-CoV (5) Serotonin Transporter (7) Sigma Receptor (1) Sodium Channel (8) TNF Receptor (1) Trace Amine-associated Receptor (TAAR) (1) Transmembrane Glycoprotein (4) Trk Receptor (4) TRP Channel (2) VEGFR (1)
By Research Areas:	Cancer (47) Cardiovascular Disease (13) Endocrinology (115) Infection (25) Inflammation/Immunology (192) Metabolic Disease (11) Neurological Disease (105)

By Targets:

5-HT Receptor (23)

Adrenergic Receptor (23)

Akt (1)

Amyloid-β (6)

Antibiotic (1)

Apoptosis (19)

Autophagy (2)

Bacterial (11)

Calcium Channel (5)

CCR (2)

CDK (1)

Checkpoint Kinase (Chk) (1)

CXCR (6)

Cytochrome P450 (5)

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Dopamine Receptor (13)

Dopamine Transporter (4)

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Drug Intermediate (2)

Drug Metabolite (8)

Endogenous Metabolite (22)

Environmental Pollutants (1)

ERK (5)

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HBV (4)

Histamine Receptor (251)

iGluR (2)

Influenza Virus (8)

Integrin (3)

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Isotope-Labeled Compounds (49)

Leukotriene Receptor (1)

Lipoxygenase (1)

mAChR (16)

Macrophage migration inhibitory factor (MIF) (1)

mGluR (3)

MOFs (1)

Neurotensin Receptor (3)

Opioid Receptor (5)

P-glycoprotein (1)

p38 MAPK (6)

Parasite (3)

PARP (1)

Potassium Channel (14)

Reference Standards (67)

SARS-CoV (5)

Serotonin Transporter (7)

Sigma Receptor (1)

Sodium Channel (8)

TNF Receptor (1)

Trace Amine-associated Receptor (TAAR) (1)

Transmembrane Glycoprotein (4)

Trk Receptor (4)

TRP Channel (2)

VEGFR (1)

By Research Areas:

Cancer (47)

Cardiovascular Disease (13)

Endocrinology (115)

Infection (25)

Inflammation/Immunology (192)

Metabolic Disease (11)

Neurological Disease (105)

275

Inhibitors & Agonists

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17043

Loratadine 10+ Cited Publications Loratidine; SCH 29851	Flavivirus Dengue Virus Histamine Receptor	Infection Inflammation/Immunology Endocrinology Cancer
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-17042

Cetirizine 3 Publications Verification	Histamine Receptor	Inflammation/Immunology Endocrinology
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] .

HY-B0303

Diphenhydramine 5+ Cited Publications	Histamine Receptor Bacterial Endogenous Metabolite iGluR	Neurological Disease Inflammation/Immunology Cancer
Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) ^[1] .

HY-B0303A

Diphenhydramine hydrochloride 5+ Cited Publications	Histamine Receptor Endogenous Metabolite Bacterial Apoptosis	Inflammation/Immunology Endocrinology Cancer
Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) ^[1] .

HY-12532

Astemizole 5+ Cited Publications R 43512	Histamine Receptor Potassium Channel	Inflammation/Immunology Endocrinology
Astemizole (R 43512), a second-generation antihistamine agent 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 ^[1] .

HY-B1281

Mepyramine maleate 2 Publications Verification Pyrilamine maleate	Histamine Receptor	Neurological Disease Endocrinology
Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with K_ds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pK_d of 9.4 for H1 receptor.

HY-B0286A

Chlorpheniramine maleate 4 Publications Verification Chlorphenamine maleate	Histamine Receptor	Inflammation/Immunology Endocrinology
Chlorpheniramine maleate is a histamine *H1 receptor* antagonist with an IC₅₀ of 12 nM ^[1] .

HY-17042A

Cetirizine dihydrochloride 3 Publications Verification P071	Histamine Receptor	Inflammation/Immunology Endocrinology Cancer
Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine *H1-receptor* antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response ^[1] .

HY-W010841

Levocetirizine dihydrochloride 2 Publications Verification (R)-Cetirizine dihydrochloride	Histamine Receptor	Inflammation/Immunology Endocrinology Cancer
Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria ^[1].

HY-14447

Bilastine	Histamine Receptor	Inflammation/Immunology Endocrinology
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 ^[1] .

HY-B0814

Levocetirizine 2 Publications Verification (R)-Cetirizine	Histamine Receptor	Inflammation/Immunology Endocrinology Cancer
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-B0548A

Hydroxyzine dihydrochloride 1 Publications Verification	Histamine Receptor	Inflammation/Immunology Endocrinology
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 ^[1] .

HY-14277A

Levocabastine hydrochloride R 50547 hydrochloride	Histamine Receptor Neurotensin Receptor Integrin	Inflammation/Immunology
Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity *neurotensin receptor* subtype 2 (NTR2) antagonist, with a K_i of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4** antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) ^[1] .

HY-B1303A

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

HY-B1794

Thiethylperazine 3 Publications Verification	Dopamine Receptor Histamine Receptor Bacterial Amyloid-β	Infection Neurological Disease
Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective *ABCC1*activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects ^[1] .

HY-121356

Carebastine 1 Publications Verification	Histamine Receptor Macrophage migration inhibitory factor (MIF) VEGFR Akt Interleukin Related	Cardiovascular Disease Inflammation/Immunology
Carebastine is an Ebastine (HY-B0674) metabolite and *H1-receptor* antagonist. Carebastine inhibits VEGFR-2 and Akt phosphorylation. Carebastine exerts an anti-inflammatory effect by inhibiting MIF as well as TNF-α and IL-6 production. Carebastine shows anti-angiogenic activity ^[1]

HY-B1303

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

HY-B0970

Diphenylpyraline hydrochloride 4-Diphenylmethoxy-1-methylpiperidine hydrochloride	Histamine Receptor	Neurological Disease Endocrinology
Diphenylpyraline hydrochloride is a potent histamine H₁?receptor antagonist. Diphenylpyraline hydrochloride acts as an orally active antihistamine agent?with antimuscarinic and antiallergic effects. Diphenylpyraline hydrochloride can be used for the relief of allergic conditions including rhinitis and hay fever, and in pruritic skin disorders in vivo. ^[1]

HY-B1483

Methapyrilene hydrochloride Thenylpyramine hydrochloride	Environmental Pollutants Histamine Receptor	Inflammation/Immunology
Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo

HY-B0303AS

Diphenhydramine-d6 hydrochloride	Isotope-Labeled Compounds Histamine Receptor Endogenous Metabolite	Inflammation/Immunology Endocrinology
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) ^[1] .

HY-136587

Oxomemazine	Histamine Receptor mGluR	Inflammation/Immunology
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (K_i= 84 nM, M1 receptor) and low (K_i= 1.65 μM, M2 receptor) affinity sites. Oxomemazine is an antihistamine and anticholinergic agent used for the study of cough treatment. Oxomemazine is protective against anaphylactic microshock in guinea pigs ^[1] .

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 ^[1] .

HY-17043S1

Loratadine-d5 Loratidine-d₅; SCH 29851-d₅	Isotope-Labeled Compounds Histamine Receptor	Infection Inflammation/Immunology Endocrinology
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-12394

Dothiepin Dosulepin; Dothep	Histamine Receptor 5-HT Receptor	Neurological Disease
Dothiepin (Dosulepin; Dothep) is an antidepressant agent with sedative/anxiolytic activity. Dothiepin is an inhibitor preferring of noradrenaline uptake than serotonin uptake. Dothiepin facilitates noradrenergic neurotransmission via inhibiting the neuronal uptake. Dothiepin is also an antagonist of histamine H1-receptor without cardiotoxicity. Dothiepin exhibits significant analgesic activity in psychogenic facial pain，idiopathic fibromyalgia syndrome or rheumatoid arthritis ^[1].

HY-B0303AS1

Diphenhydramine-d5 hydrochloride	Histamine Receptor Endogenous Metabolite	Inflammation/Immunology Endocrinology
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) ^[1] .

HY-B0303R

Diphenhydramine (Standard)	Reference Standards Histamine Receptor Bacterial Endogenous Metabolite iGluR	Neurological Disease Inflammation/Immunology Cancer
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) ^[1] .

HY-17042S1

Cetirizine-d8	Histamine Receptor	Inflammation/Immunology
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 ^[1] .

HY-17043R

Loratadine (Standard) Loratidine (Standard); SCH 29851 (Standard)	Dengue Virus Flavivirus Reference Standards Histamine Receptor	Infection Inflammation/Immunology Endocrinology Cancer
Loratadine (Standard) is the analytical standard of Loratadine. This product is intended for research and analytical applications. 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-W010841R

Levocetirizine dihydrochloride (Standard) (R)-Cetirizine dihydrochloride (Standard)	Reference Standards Histamine Receptor	Inflammation/Immunology Endocrinology
Levocetirizine (dihydrochloride) (Standard) is the analytical standard of Levocetirizine (dihydrochloride). This product is intended for research and analytical applications. Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria ^[1].

HY-B0303AR

Diphenhydramine hydrochloride (Standard) 5 Publications Verification	Reference Standards Histamine Receptor Endogenous Metabolite Bacterial	Inflammation/Immunology Endocrinology Cancer
Diphenhydramine (hydrochloride) (Standard) is the analytical standard of Diphenhydramine (hydrochloride). This product is intended for research and analytical applications. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) ^[1] .

HY-107647A

(R)-(+)-Dimethindene maleate	Histamine Receptor	Inflammation/Immunology
(R)-(+)-Dimethindene maleate is an orally active *H₁-receptor* blocker with antihistaminic properties in pigs ^[1].

HY-B0814R

Levocetirizine (Standard) (R)-Cetirizine (Standard)	Histamine Receptor Reference Standards	Inflammation/Immunology Endocrinology Cancer
Levocetirizine (Standard) is the analytical standard of Levocetirizine. This product is intended for research and analytical applications. 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-B0814S1

Levocetirizine-d4 (R)-Cetirizine-d₄	Isotope-Labeled Compounds	Inflammation/Immunology
Levocetirizine-d₄ ((R)-Cetirizine-d₄) is the deuterium-labeled Levocetirizine (HY-B0814) ^[1]. 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-122508

Hydroxyebastine	Drug Metabolite	Neurological Disease
Hydroxyebastine is an Ebastine (HY-B0674) (a histamine H₁-receptor antagonist) metabolite. Hydroxyebastine is metabolized to Carebastine (HY-121356) by CYP2J2 and CYP3A4 ^[1].

HY-B0539S3

Desloratadine-d5 Sch34117-d₅	Isotope-Labeled Compounds Histamine Receptor Endogenous Metabolite	Inflammation/Immunology Endocrinology
Desloratadine-d₅ is deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities ^[1] .

HY-14277

Levocabastine R 50547	Histamine Receptor Neurotensin Receptor Integrin	Inflammation/Immunology
Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity *neurotensin receptor* subtype 2 (NTR2) antagonist, with a K_i of 17 nM for mNTR2. Levocabastine can act as a VLA-4** antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) ^[1] .

HY-12532S

Astemizole-d3	Isotope-Labeled Compounds Histamine Receptor Potassium Channel	Inflammation/Immunology Endocrinology
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 ^[1] .

HY-402545

(-)-Brompheniramine (R)-Brompheniramine	Histamine Receptor	Inflammation/Immunology
(-)-Brompheniramine is a H1 receptor antagonist with antiallergic activity ^[1].

HY-B0548S1

Hydroxyzine D8	Histamine Receptor	Inflammation/Immunology Endocrinology
Hydroxyzine-d₈ is deuterium labeled Hydroxyzine. Hydroxyzine is a histamine H1-receptor antagonist ^[1].

HY-105542

Niaprazine	Histamine Receptor	Neurological Disease
Niaprazine is a histamine H1-receptor antagonist. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research ^[1] .

HY-W660701

Bamipine	Histamine Receptor Bacterial	Infection Neurological Disease
Bamipine is a potent histamine H1-receptor antagonist. Bamipine exhibits moderate activity against Mycobacterium tuberculosis. Bamipine has a mild sedative effect ^[1] .

HY-131256

Cetirizine Impurity C	Histamine Receptor	Inflammation/Immunology Endocrinology
Cetirizine Impurity C is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist ^{[1] ^{^{[2] ^.}}}

HY-12966

Cetirizine methyl ester	Histamine Receptor	Inflammation/Immunology Endocrinology
Cetirizine methyl ester is an impurity of Cetirizine (HY-17042). Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist ^[1].

HY-17042S

Cetirizine-d4	Histamine Receptor	Inflammation/Immunology
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-B1794A

Thiethylperazine dimaleate 3 Publications Verification	Dopamine Receptor Histamine Receptor Bacterial Amyloid-β	Infection Neurological Disease
Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective *ABCC1*activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects ^[1] .

HY-12532R

Astemizole (Standard) R 43512 (Standard)	Reference Standards Histamine Receptor Potassium Channel	Inflammation/Immunology Endocrinology
Astemizole (Standard) is the analytical standard of Astemizole. This product is intended for research and analytical applications. Astemizole (R 43512), a second-generation antihistamine agent 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 ^[1] .

HY-147336

Desmethylazelastine	Drug Metabolite	Infection Cardiovascular Disease Metabolic Disease Inflammation/Immunology
Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2 ^[1] .

HY-124517

Burimamide	Histamine Receptor Adrenergic Receptor	Neurological Disease Inflammation/Immunology
Burimamide is a blocker of histamine H2-receptor. Burimamide inhibits gastric acid secretion evoked by Pentagastrin (HY-A0261) or Gastrin. Burimamide also has alpha-adrenoceptor blocking activity. Burimamide in combination with the H1-receptor antagonist Mepyramine (HY-B1281) shows anti-inflammatory activity in a rat paw edema model induced by Compound 48/80 (HY-115768) ^[1] .

HY-14145

NBI-75043	Histamine Receptor	Others
NBI-75043 is an antagonist of *H1 receptor* ^[1].

HY-101830

Wy 49051	Histamine Receptor	Inflammation/Immunology Endocrinology
Wy 49051 is a potent, orally active *H1 receptor* antagonist, with IC₅₀ of 44 nM.

Cat. No.	Product Name	Category	Target	Chemical Structure

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 ^[1] .

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 ^[1] .

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) ^[1] .

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) ^[1] .

HY-N0054

Osthole Maximum Cited Publications 16 Publications Verification 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 ^[1] .

HY-B0188A

Mianserin hydrochloride 1 Publications Verification Org GB 94	Alkaloids Structural Classification Neurological Disease Classification of Application Fields Leguminosae Other Alkaloids Crotalaria pallida Ait. Plants Disease Research Fields Endocrinology Source Classification	Histamine Receptor Opioid Receptor ERK p38 MAPK
Mianserin hydrochloride (Org GB 94) is an orally active *H1 receptor* antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases *ERK1/2* and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy ^[1] .

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 ^[1] .

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 ^[1] .

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 ^[1] .

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 ^[1] .

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 ^[1] .

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) ^[1] .

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 ^[1].

HY-B0188AR

Mianserin hydrochloride (Standard) Org GB 94 (Standard)	Alkaloids Structural Classification Leguminosae Other Alkaloids Crotalaria pallida Ait. Plants Source Classification	Reference Standards Histamine Receptor Opioid Receptor ERK p38 MAPK
Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride is an orally active *H1 receptor* antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases *ERK1/2* and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy ^[1] .

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 ^[1] .

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 ^[1] .

HY-B0539R

Desloratadine (Standard) Sch34117 (Standard)	Structural Classification Natural Products Classification of Application Fields Endogenous metabolite Disease Research Fields Endocrinology Source Classification	Histamine Receptor Endogenous Metabolite Drug Metabolite Reference Standards
Desloratadine (Standard) is the analytical standard of Desloratadine. This product is intended for research and analytical applications. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating *H1-antihistamine* Loratadine. Desloratadine is a selective *H1-receptor* antagonist that has anti-allergic and anti-inflammatory activities ^[1] .

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 ^[1] .

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 ^[1] .

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 ^[1] .

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 ^[1] .

HY-N6772R

Cytochalasin E (Standard)	Alkaloids Structural Classification Microorganisms Pyrrole Alkaloids Source Classification	Reference Standards Autophagy
Antazoline (phosphate) (Standard) is the analytical standard of Antazoline (phosphate). This product is intended for research and analytical applications. Antazoline phosphate is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect ^[1] .

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-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 ^[1] .

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 ^[1] .

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 ^[1] .

Cat. No.	Compare	Product Name	Species	Source	Image

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) ^[1] .

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) ^[1] .

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 ^[1] .

HY-B0781S

Promethazine-d4 hydrochloride
Promethazine-d₄ (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.

HY-B0527AS

Amitriptyline-d6 hydrochloride

Amitriptyline-d₆ hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-B0814S1

Levocetirizine-d4

Levocetirizine-d₄ ((R)-Cetirizine-d₄) is the deuterium-labeled Levocetirizine (HY-B0814) ^[1]. 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-B0539S3

Desloratadine-d5
Desloratadine-d₅ is deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities ^[1] .

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 ^[1] .

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 ^[1] .

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-B0188S

Mianserin-d3

Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy ^[1] .

HY-B0548S1

Hydroxyzine D8
Hydroxyzine-d₈ is deuterium labeled Hydroxyzine. Hydroxyzine is a histamine H1-receptor antagonist ^[1].

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-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 ^[1] .

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 ^[1] .

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 ^[1] .

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 ^[1] .

HY-B0188AS

Mianserin-d3 hydrochloride

Mianserin-d₃ hydrochloride is the deuterium labeled Mianserin. Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy ^[1] .

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-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 ^[1].

HY-B0539S1

Desloratadine-d9
Desloratadine-d₉ is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities ^[1] .

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-B0539S

Desloratadine-d4
Desloratadine-d₄ is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].

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 ^[1] .

HY-17042AS1

Cetirizine-d8 dihydrochloride
Cetirizine-d₈ (dihydrochloride) 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] .

HY-17042AS

Cetirizine-d4 dihydrochloride
Cetirizine-d₄ (dihydrochloride) 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] .

HY-B0539S4

Desloratadine-d4 hydrobromide
Desloratadine-d₄ hydrobromide is deuterated labeled Desloratadine (HY-B0539). Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating *H1-antihistamine* Loratadine. Desloratadine is a selective *H1-receptor* antagonist that has anti-allergic and anti-inflammatory activities ^[1] .

HY-23188

Loratadine-d5-1
Loratadine-d₅-1 is a deuterated labeled Loratadine (HY-17043). 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-17043S2

Loratadine-d4-1
Loratadine-d₄-1 (Loratidine-d₄-1) is 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 ^[1].

HY-B0539S2

Desloratadine-3,3,5,5-d4
Desloratadine-3,3,5,5-d₄ is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].

HY-17043S3

Loratadine-13C6
Loratadine- ¹³C₆ (SCH 29851- ¹³C₆) is ¹³C 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-B1794S

Thiethylperazine-d3
Thiethylperazine-d₃ is the deuterium labeled Thiethylperazinee (HY-B1794). Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects ^[1] .

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-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 ^[1] .

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 ^[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA) .

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 ^[1] .

HY-B0801S2

Fexofenadine-d3
Fexofenadine-d₃ is the deuterium labeled Fexofenadine ^[1]. Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research .

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 ^[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA) .

HY-B0674S

Ebastine-d5
Ebastine-d₅ is the deuterium labeled Ebastine. Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research ^[1] .

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 ^[1] .

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 ^[1] .

HY-B0674S1

Ebastine-d6
Ebastine-d₆ is deuterated labeled Ebastine (HY-B0674). Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research ^[1].

HY-B0801S4

Fexofenadine-d3-1
Fexofenadine-d₃-1 fumarate is deuterated labeled Fexofenadine (HY-B0801). Fexofenadine (MDL-16455) is an orally active and nonsedative *H1 receptor* antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research ^[1] .

HY-B1296S1

Promethazine-d4
Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties ^[1] .

HY-121356S

Carebastine-d5
Carebastine-d₅ is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner ^[1]. Carebastine suppresses the expression of macrophage migration inhibitory factor .

HY-121356S1

Carebastine-d5 Methyl Ester
Carebastine-d₅ Methyl Ester is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner ^[1]. Carebastine suppresses the expression of macrophage migration inhibitory factor .

HY-108411S

Emedastine-13C,d3 fumarate
Emedastine- ¹³C,d₃ fumarate is the ¹³C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a K_i value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis ^[1] .

HY-A0015S

Bepotastine-d6 besylate
Bepotastine-d₆(besylate) is deuterium labeled Bepotastine (besilate). Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research ^[1] .

HY-B0781S1

Promethazine-d3 hydrochloride

Promethazine-d₃ (hydrochloride) is deuterium labeled Promethazine (hydrochloride). Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors ^[1] .

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