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Results for "

H1 histamine receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Histamine Receptor (189) 5-HT Receptor (23) Adrenergic Receptor (13) Amyloid-β (2) Apoptosis (12) Autophagy (2) Bacterial (6) Calcium Channel (4) Caspase (2) Cytochrome P450 (4) Dengue virus (2) Dopamine Receptor (12) Drug Metabolite (3) Endogenous Metabolite (19) FAK (2) Flavivirus (2) HBV (2) HCV (3) HCV Protease (2) iGluR (3) Influenza Virus (3) Integrin (3) Isotope-Labeled Compounds (23) Leukotriene Receptor (1) Lipoxygenase (1) mAChR (6) Macrophage migration inhibitory factor (MIF) (1) mGluR (1) Na+/Ca2+ Exchanger (2) Neurotensin Receptor (3) P2X Receptor (2) Parasite (2) Phosphodiesterase (PDE) (3) Potassium Channel (9) SARS-CoV (3) Sigma Receptor (1) Sodium Channel (4) STAT (1) TNF Receptor (1) TRP Channel (3) VEGFR (2)
By Research Areas:	Cancer (33) Cardiovascular Disease (8) Endocrinology (105) Infection (10) Inflammation/Immunology (154) Metabolic Disease (2) Neurological Disease (64)

By Targets:

Histamine Receptor (189)

5-HT Receptor (23)

Adrenergic Receptor (13)

Amyloid-β (2)

Apoptosis (12)

Autophagy (2)

Bacterial (6)

Calcium Channel (4)

Caspase (2)

Cytochrome P450 (4)

Dengue virus (2)

Dopamine Receptor (12)

Drug Metabolite (3)

Endogenous Metabolite (19)

FAK (2)

Flavivirus (2)

HBV (2)

HCV (3)

HCV Protease (2)

iGluR (3)

Influenza Virus (3)

Integrin (3)

Isotope-Labeled Compounds (23)

Leukotriene Receptor (1)

Lipoxygenase (1)

mAChR (6)

Macrophage migration inhibitory factor (MIF) (1)

mGluR (1)

Na+/Ca2+ Exchanger (2)

Neurotensin Receptor (3)

P2X Receptor (2)

Parasite (2)

Phosphodiesterase (PDE) (3)

Potassium Channel (9)

SARS-CoV (3)

Sigma Receptor (1)

Sodium Channel (4)

STAT (1)

TNF Receptor (1)

TRP Channel (3)

VEGFR (2)

By Research Areas:

Cancer (33)

Cardiovascular Disease (8)

Endocrinology (105)

Infection (10)

Inflammation/Immunology (154)

Metabolic Disease (2)

Neurological Disease (64)

211

Inhibitors & Agonists

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Targets Recommended: Histamine Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-A0191

Dexbrompheniramine (+)-Brompheniramine; (S)-Brompheniramine	Endogenous Metabolite Histamine Receptor	Inflammation/Immunology
Dexbrompheniramine is an orally active H1 receptor antagonist. Dexbrompheniramine is an antihistamine that reduces the effects of natural chemical histamine. Dexbrompheniramine can be used for the research of hay fever and urticaria .

HY-B1589A

Carbinoxamine maleate salt 1 Publications Verification	Histamine Receptor	Neurological Disease Endocrinology
Carbinoxamine maleate salt is a **histamine H1 receptor** antagonist.

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_d*s 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-B1303A

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

HY-B1303

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

HY-A0191A

Dexbrompheniramine maleate (+)-Brompheniramine maleate; (S)-Brompheniramine maleate	Endogenous Metabolite Histamine Receptor	Inflammation/Immunology
Dexbrompheniramine maleate is an orally active H1 receptor antagonist. Dexbrompheniramine maleate is an antihistamine that reduces the effects of natural chemical histamine. Dexbrompheniramine maleate can be used for the research of hay fever and urticaria .

HY-100280

Pirolate CP-32387	Histamine Receptor	Inflammation/Immunology Endocrinology
Pirolate is a histamine H1 receptor antagonist.

HY-B1589

(±)-Carbinoxamine	Histamine Receptor	Neurological Disease
(±)-Carbinoxamine is a **histamine H1 receptor** antagonist .

HY-129783

Phenindamine tartrate	Histamine Receptor	Inflammation/Immunology
Phenindamine tartrate is a **Histamine H1-receptor** antagonist. Phenindamine tartrate is an antihistamine .

HY-B0298A

Clemastine fumarate 5+ Cited Publications HS-592 fumarate; Meclastine fumarate	Histamine Receptor	Neurological Disease Endocrinology
Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .

HY-B0298

Clemastine HS-592; Meclastine	Histamine Receptor	Neurological Disease
Clemastine (HS-592) is a potent and orally active histamine receptor H1 antagonist. Clemastine is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .

HY-U00018

(±)-Tazifylline	Histamine Receptor	Neurological Disease Endocrinology
(±)-Tazifylline is a potent, selective and long-acting **histamine H1 receptor** antagonist.

HY-B1281R

Mepyramine maleate (Standard)	Histamine Receptor	Neurological Disease Endocrinology
Mepyramine maleate (Standard) is the analytical standard of Mepyramine maleate. This product is intended for research and analytical applications. Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pKd of 9.4 for H1 receptor.

HY-101724

ReN-1869 hydrochloride NNC-05-1869 hydrochloride	Histamine Receptor	Inflammation/Immunology Endocrinology
ReN 1869 hydrochloride is a novel, selective **histamine H₁ receptor** antagonist, which demonstrates affinity to the histamine H₁ receptor (guinea pig brain) with K_i of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with K_i of 0.45 μM.

HY-B0286A

Chlorpheniramine maleate 2 Publications Verification Chlorphenamine maleate	Histamine Receptor	Inflammation/Immunology Endocrinology
Chlorpheniramine maleate is a histamine H1 receptor antagonist with an IC₅₀ of 12 nM .

HY-B0548S1

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

HY-B1589AS

Carbinoxamine-d6 maleate	Isotope-Labeled Compounds Histamine Receptor	Neurological Disease Endocrinology
Carbinoxamine-d₆ (maleate) is the deuterium labeled Carbinoxamine maleate salt. Carbinoxamine maleate salt is a histamine H1 receptor antagonist.

HY-B0814

Levocetirizine 1 Publications Verification (R)-Cetirizine	Histamine Receptor	Inflammation/Immunology Endocrinology
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-W010841

Levocetirizine dihydrochloride 1 Publications Verification (R)-Cetirizine dihydrochloride	Histamine Receptor	Inflammation/Immunology Endocrinology
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 .

HY-B0298AR

Clemastine fumarate (Standard) HS-592 fumarate (Standard); Meclastine fumarate (Standard)	Histamine Receptor	Neurological Disease Endocrinology
Clemastine (fumarate) (Standard) is the analytical standard of Clemastine (fumarate). This product is intended for research and analytical applications. Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .

HY-A0178A

Isothipendyl hydrochloride NSC 169186	Endogenous Metabolite Histamine Receptor	Inflammation/Immunology
Isothipendyl hydrochloride (), an azaphenothiazine derivative, is a potent **histamine 1 (H1)** receptor antagonist.othipendyl is a primary metabolite .

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 .

HY-123829

LY2624803	Histamine Receptor 5-HT Receptor	Inflammation/Immunology
LY2624803 is a 5-HT2A and histamine, H1 receptor antagonist .

HY-17039

Alcaftadine R89674	Histamine Receptor	Inflammation/Immunology Endocrinology
Alcaftadine (R89674) is a **histamine H1 receptor** antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis. Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects .

HY-19489S

(±)-Levomepromazine-d6 (±)-Methotrimeprazine-d₆; dl-Methotrimeprazine-d₆	Dopamine Receptor Histamine Receptor	Neurological Disease
(±)-Levomepromazine-d₆ is the deuterium labeled Methotrimeprazine, which is a D3 dopamine and Histamine H1 receptor antagonist.

HY-B1305

Chloropyramine hydrochloride	FAK Histamine Receptor VEGFR	Endocrinology Cancer
Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.

HY-A0178

Isothipendyl AY 56012	Histamine Receptor Endogenous Metabolite	Inflammation/Immunology
Isothipendyl (AY 56012), an azaphenothiazine derivative, is a potent **histamine 1 (H1)** receptor antagonist. Isothipendyl is a primary metabolite .

HY-B1589AR

Carbinoxamine maleate salt (Standard)	Histamine Receptor	Neurological Disease Endocrinology
Carbinoxamine maleate salt (Standard) is the analytical standard of Carbinoxamine maleate salt. This product is intended for research and analytical applications. Carbinoxamine maleate salt is a **histamine H1 receptor** antagonist.

HY-B0303A

Diphenhydramine hydrochloride 5 Publications Verification	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) .

HY-17428

Tripelennamine hydrochloride	Histamine Receptor Endogenous Metabolite	Inflammation/Immunology Endocrinology
Tripelennamine hydrochloride, an ethylenediamine derivative, is a potent histamine *H1-receptor* antagonist. Tripelennamine hydrochloride lessens the allergic response of the organism caused by histamine. Tripelennamine hydrochloride can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .

HY-17428A

Tripelennamine	Histamine Receptor Endogenous Metabolite	Inflammation/Immunology Endocrinology
Tripelennamine, an ethylenediamine derivative, is a potent histamine *H1-receptor* antagonist. Tripelennamine lessens the allergic response of the organism caused by histamine. Tripelennamine can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .

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-B0814S

Levocetirizine-d4 dihydrochloride (R)-Cetirizine-d₄(dihydrochloride)	Isotope-Labeled Compounds Histamine Receptor	Inflammation/Immunology Endocrinology
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	Histamine Receptor	Neurological Disease Inflammation/Immunology Endocrinology
Hydroxyzine-d₄ (dihydrochloride) is deuterium labeled Hydroxyzine. Hydroxyzine is a heterocyclic histamine H1-receptor antagonist. Hydroxyzine has anticholinergic, anxiolytic and analgesic properties[1].

HY-B0303

Diphenhydramine 5 Publications Verification	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) .

HY-B0524A

Betahistine dihydrochloride	Histamine Receptor	Neurological Disease Inflammation/Immunology Endocrinology
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-B0524

Betahistine	Histamine Receptor	Inflammation/Immunology Cancer
Betahistine is an orally active **histamine H1 receptor** agonist and a H3 receptor antagonist . Betahistine is used for the study of rheumatoid arthritis (RA) .

HY-D0237

Betahistine mesylate	Histamine Receptor	Inflammation/Immunology
Betahistine mesylate is an orally active **histamine H1 receptor** agonist and a H3 receptor antagonist . Betahistine mesylate is used for the study of rheumatoid arthritis (RA) .

HY-W010841R

Levocetirizine dihydrochloride (Standard) (R)-Cetirizine dihydrochloride (Standard)	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 .

HY-B0895

Hydroxyzine pamoate	Histamine Receptor	Inflammation/Immunology Endocrinology
Hydroxyzine pamoate is a histamine receptor H1 antagonist, one of the salt forms of Hydroxyzine, soluble in dimethyl formamide and chloroform but insoluble in water and alcohol .

HY-17428B

Tripelennamine citrate	Histamine Receptor Endogenous Metabolite	Inflammation/Immunology Endocrinology
Tripelennamine citrate, an ethylenediamine derivative, is a potent histamine *H1-receptor* antagonist. Tripelennamine citrate lessens the allergic response of the organism caused by histamine. Tripelennamine citrate can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .

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-131256A

Cetirizine Impurity C dihydrochloride	Histamine Receptor	Inflammation/Immunology Endocrinology
Cetirizine Impurity C dihydrochloride 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-B0298AS

Clemastine-d5 fumarate 1 Publications Verification HS-592-d5 (fumarate); Meclastine-d5 (fumarate)	Histamine Receptor Autophagy	Neurological Disease Endocrinology
Clemastine-d₅ (fumarate) is the deuterium labeled Clemastine fumarate. Clemastine fumarate (HS-592 fumarate) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.

HY-B0895R

Hydroxyzine pamoate (Standard)	Histamine Receptor	Inflammation/Immunology Endocrinology
Hydroxyzine (pamoate) (Standard) is the analytical standard of Hydroxyzine (pamoate). This product is intended for research and analytical applications. Hydroxyzine pamoate is a histamine receptor H1 antagonist.

HY-17039R

Alcaftadine (Standard)	Histamine Receptor	Inflammation/Immunology Endocrinology
Alcaftadine (Standard) is the analytical standard of Alcaftadine. This product is intended for research and analytical applications. Alcaftadine (R89674) is a **histamine H1 receptor** antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis. Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects .

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 .

HY-N0054

Osthole Maximum Cited Publications 11 Publications Verification Osthol; NSC 31868	Histamine Receptor Apoptosis Parasite HBV	Infection Cardiovascular Disease Inflammation/Immunology Endocrinology Cancer
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-B1303R

Mebhydrolin napadisylate (Standard)	Histamine Receptor	Inflammation/Immunology Endocrinology
Mebhydrolin (napadisylate) (Standard) is the analytical standard of Mebhydrolin (napadisylate). This product is intended for research and analytical applications. Mebhydrolin napadisylate is a specific **histamine H₁ receptor** antagonist.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-A0191

Dexbrompheniramine (+)-Brompheniramine; (S)-Brompheniramine	Structural Classification Natural Products Classification of Application Fields Source classification Endogenous metabolite Inflammation/Immunology Disease Research Fields	Endogenous Metabolite Histamine Receptor
Dexbrompheniramine is an orally active H1 receptor antagonist. Dexbrompheniramine is an antihistamine that reduces the effects of natural chemical histamine. Dexbrompheniramine can be used for the research of hay fever and urticaria .

HY-B0303A

Diphenhydramine hydrochloride 5 Publications Verification	Structural Classification Alkaloids Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Inflammation/Immunology Disease Research Fields	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-17428

Tripelennamine hydrochloride	Structural Classification Alkaloids Classification of Application Fields Source classification Pyridine Alkaloids Endogenous metabolite Inflammation/Immunology Disease Research Fields	Histamine Receptor Endogenous Metabolite
Tripelennamine hydrochloride, an ethylenediamine derivative, is a potent histamine *H1-receptor* antagonist. Tripelennamine hydrochloride lessens the allergic response of the organism caused by histamine. Tripelennamine hydrochloride can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .

HY-B0303

Diphenhydramine 5 Publications Verification	Structural Classification Alkaloids Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Inflammation/Immunology Disease Research Fields	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-N0054

Osthole Maximum Cited Publications 11 Publications Verification Osthol; NSC 31868	Cardiovascular Disease Structural Classification Classification of Application Fields Source classification Coumarins Plants Biological Pesticide Research Agricultural Research Infection other families Phenylpropanoids Inflammation/Immunology Disease Research Fields Endocrinology	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-17042

Cetirizine 2 Publications Verification	Classification of Application Fields Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields Endocrinology	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-A0178

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

HY-17428A

Tripelennamine	Structural Classification Alkaloids Classification of Application Fields Source classification Pyridine Alkaloids Endogenous metabolite Inflammation/Immunology Disease Research Fields Endocrinology	Histamine Receptor Endogenous Metabolite
Tripelennamine, an ethylenediamine derivative, is a potent histamine *H1-receptor* antagonist. Tripelennamine lessens the allergic response of the organism caused by histamine. Tripelennamine can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .

HY-17428B

Tripelennamine citrate	Structural Classification Alkaloids Classification of Application Fields Source classification Pyridine Alkaloids Endogenous metabolite Inflammation/Immunology Disease Research Fields Endocrinology	Histamine Receptor Endogenous Metabolite
Tripelennamine citrate, an ethylenediamine derivative, is a potent histamine *H1-receptor* antagonist. Tripelennamine citrate lessens the allergic response of the organism caused by histamine. Tripelennamine citrate can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .

HY-17428R

Tripelennamine hydrochloride (Standard)	Structural Classification Alkaloids Source classification Pyridine Alkaloids Endogenous metabolite	Histamine Receptor Endogenous Metabolite
Tripelennamine (hydrochloride) (Standard) is the analytical standard of Tripelennamine (hydrochloride). This product is intended for research and analytical applications. Tripelennamine hydrochloride, an ethylenediamine derivative, is a potent histamine *H1-receptor* antagonist. Tripelennamine hydrochloride lessens the allergic response of the organism caused by histamine. Tripelennamine hydrochloride can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .

HY-B0303R

Diphenhydramine (Standard)	Structural Classification Alkaloids Other Alkaloids Source classification Endogenous metabolite	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-N0054R

Osthole (Standard)	Structural Classification other families Source classification Coumarins Phenylpropanoids Plants	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 Source classification Endogenous metabolite	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-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-W062109

Olopatadine	Structural Classification Alkaloids Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Inflammation/Immunology Disease Research Fields	Endogenous Metabolite Histamine Receptor
Olopatadine is an orally active and selective **histamine 1 (H₁) receptor** antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis .

HY-B0157A

Ketotifen fumarate 3 Publications Verification HC 20511 fumarate	Structural Classification Natural Products Classification of Application Fields Source classification Endogenous metabolite Inflammation/Immunology Disease Research Fields	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-B0157

Ketotifen 3 Publications Verification HC 20-511	Infection Structural Classification Natural Products Classification of Application Fields Source classification Endogenous metabolite Inflammation/Immunology Disease Research Fields Endocrinology	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-B0539

Desloratadine 5+ 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-B0157AR

Ketotifen fumarate (Standard)	Structural Classification Natural Products Source classification Endogenous metabolite	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 .

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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. The total length of HRH1 Protein, Human (His) is 206 a.a.,

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Cat. No.	Product Name	Chemical Structure

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-B0548S1

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

HY-19489S

(±)-Levomepromazine-d6
(±)-Levomepromazine-d₆ is the deuterium labeled Methotrimeprazine, which is a D3 dopamine and Histamine H1 receptor antagonist.

HY-B0298AS

Clemastine-d5 fumarate 1 Publications Verification
Clemastine-d₅ (fumarate) is the deuterium labeled Clemastine fumarate. Clemastine fumarate (HS-592 fumarate) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.

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][2].

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][2].

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-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-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-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][2].

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)[3].

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-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-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)[3].

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][2][3].

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][2][3].

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-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][2][3].

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][2][3].

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][2].

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][2].

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][2].

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 .

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[1][2].

HY-12752BS

Alimemazine-d6 hydrochloride

Alimemazine-d6 hydrochloride (Trimeprazine-d6 hydrochloride) is the deuterium labeled Alimemazine (HY-12752). Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .

HY-A0027AS

Fenspiride-d5

Fenspiride-d₅ is the deuterium labeled Fenspiride. 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[1][2][3].

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[2].

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[2].

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 Ki 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][2][3].

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][2][3][4].

HY-W062109S

Olopatadine-d6
Olopatadine-d₆ is the deuterium labeled Olopatadine[1]. Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis[2][3].

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-B0352S2

Mirtazapine-d4
Mirtazapine-d₄ is deuterium labeled Mirtazapine. 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 pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].

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-10564S

Sarpogrelate-d3 hydrochloride

Sarpogrelate-d₃ (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].

HY-B1658BS

Frovatriptan-d3 succinate

Frovatriptan-d₃ (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].

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