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Histamine Receptor Antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Histamine Receptor (308) 5-HT Receptor (28) Adenylate Cyclase (1) Adrenergic Receptor (21) Amyloid-β (3) Apoptosis (15) Autophagy (5) Bacterial (19) Calcium Channel (5) Caspase (3) Cholinesterase (ChE) (3) Cytochrome P450 (8) Dopamine Receptor (31) Drug Metabolite (5) Endogenous Metabolite (16) FAK (2) Ferroptosis (1) Filovirus (1) GnRH Receptor (1) HCV (3) HCV Protease (2) iGluR (3) Influenza Virus (1) Integrin (3) Isotope-Labeled Compounds (27) Leukotriene Receptor (1) Lipoxygenase (1) mAChR (13) Macrophage migration inhibitory factor (MIF) (1) mGluR (1) Monoamine Oxidase (1) Na+/Ca2+ Exchanger (2) Neurokinin Receptor (1) Neurotensin Receptor (3) NF-κB (1) P2X Receptor (2) p38 MAPK (1) Parasite (2) Phosphodiesterase (PDE) (3) Potassium Channel (9) Reactive Oxygen Species (1) SARS-CoV (1) Serotonin Transporter (1) Sigma Receptor (4) Sodium Channel (4) Tau Protein (1) TNF Receptor (1) TRP Channel (3) VEGFR (2)
By Research Areas:	Cancer (55) Cardiovascular Disease (5) Endocrinology (151) Infection (12) Inflammation/Immunology (179) Metabolic Disease (21) Neurological Disease (130)

By Targets:

Histamine Receptor (308)

5-HT Receptor (28)

Adenylate Cyclase (1)

Adrenergic Receptor (21)

Amyloid-β (3)

Apoptosis (15)

Autophagy (5)

Bacterial (19)

Calcium Channel (5)

Caspase (3)

Cholinesterase (ChE) (3)

Cytochrome P450 (8)

Dopamine Receptor (31)

Drug Metabolite (5)

Endogenous Metabolite (16)

FAK (2)

Ferroptosis (1)

Filovirus (1)

GnRH Receptor (1)

HCV (3)

HCV Protease (2)

iGluR (3)

Influenza Virus (1)

Integrin (3)

Isotope-Labeled Compounds (27)

Leukotriene Receptor (1)

Lipoxygenase (1)

mAChR (13)

Macrophage migration inhibitory factor (MIF) (1)

mGluR (1)

Monoamine Oxidase (1)

Na+/Ca2+ Exchanger (2)

Neurokinin Receptor (1)

Neurotensin Receptor (3)

NF-κB (1)

P2X Receptor (2)

p38 MAPK (1)

Parasite (2)

Phosphodiesterase (PDE) (3)

Potassium Channel (9)

Reactive Oxygen Species (1)

SARS-CoV (1)

Serotonin Transporter (1)

Sigma Receptor (4)

Sodium Channel (4)

Tau Protein (1)

TNF Receptor (1)

TRP Channel (3)

VEGFR (2)

By Research Areas:

Cancer (55)

Cardiovascular Disease (5)

Endocrinology (151)

Infection (12)

Inflammation/Immunology (179)

Metabolic Disease (21)

Neurological Disease (130)

335

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Histamine Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-145106

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

HY-B1296

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

HY-115833

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

HY-107557

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

HY-107557A

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

HY-19010

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

HY-116560

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

HY-107556

VUF 5681 dihydrobromide	Histamine Receptor	Neurological Disease
VUF 5681 dihydrobromide is a neutral antagonist of histamine H₃ receptor. VUF 5681 dihydrobromide also has partial agonist function of H₃ receptor. VUF 5681 dihydrobromide blocks the effects of Thioperamide (HY-12206). VUF 5681 dihydrobromide is used in central nervous system disease research .

HY-119087

JNJ-28583867	Histamine Receptor Serotonin Transporter	Neurological Disease
JNJ-28583867 is an orally active and selective **histamine H3 receptor** antagonist (K_i=10.6 nM) and serotonin transporter (SERT) inhibitor (K_i=3.7 nM). JNJ-28583867 can be used in the research of depression .

HY-107561

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

HY-122171

A-317920	Histamine Receptor	Neurological Disease
A-317920 is a selective and potent *rat histamine* H3 receptor (H3R)** antagonist with pK_i value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade .

HY-15539

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

HY-B1589A

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

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-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-100191

BMY-25271	Histamine Receptor	Inflammation/Immunology Endocrinology
BMY-25271 is a **histamine H2 receptor** antagonist.

HY-142090

Donetidine SK&F 93574	Histamine Receptor	Others
Donetidine (SK&F 93574) is an antagonist for **histamine H2 receptor*, that promotes histamine* release in beagle dog models .

HY-B0548S1

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

HY-117981

OUP-186	Histamine Receptor	Inflammation/Immunology
OUP-186 is a histamine H3 receptor antagonist .

HY-117500

Aplysamine-1	Others	Inflammation/Immunology
Aplysamine-1 acts as an antagonist for the histamine H3 receptor.

HY-15540

Metiamide SK&F 92058	Histamine Receptor	Endocrinology
Metiamide (SK&F 92058) is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide.

HY-156667

H4R antagonist 3	Histamine Receptor	Inflammation/Immunology
H4R antagonist 3 (Example 18) is a **histamine-4 receptor** antagonist with an EC₅₀ of ＜10 mM. H4R antagonist 3 can be used for the research of prevention of inflammatory, autoimmune, allergic, and ocular diseases .

HY-129783

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

HY-U00018

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

HY-17582

Decloxizine 1 Publications Verification UCB-1402; NSC289116	Histamine Receptor	Inflammation/Immunology Endocrinology
Decloxizine(UCB-1402; NSC289116) is a histamine 1 receptor antagonist.

HY-12191A

A 331440 hydrochloride	Histamine Receptor	Metabolic Disease
A 331440 hydrochloride is a **histamine H3 receptor** antagonist. A 331440 hydrochloride binds potently and selectively to human and rat histamine H3 receptors (K_i≤25 nM). A 331440 hydrochloride can be used for antiobesity research .

HY-122148

DA 4626	Adenylate Cyclase Histamine Receptor	Metabolic Disease
DA 4626 is a competitive *H2-histamine* receptor antagonist. DA 4626 inhibits adenylate cyclase activity with a K_B value of 40 nM .

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-A0075

Decloxizine dihydrochloride 1 Publications Verification UCB 1402 dihydrochloride	Histamine Receptor	Inflammation/Immunology Endocrinology
Decloxizine dihydrochloride(UCB-1402; NSC289116) is a histamine 1 receptor antagonist.

HY-109074

Seliforant SENS-111	Histamine Receptor	Inflammation/Immunology
Seliforant (SENS-111) is a selective and orally **histamine H4 receptor** antagonist.

HY-B1296S

Promethazine-d6 hydrochloride (±)-Promethazine-d₆ (hydrochloride)	Histamine Receptor	Neurological Disease
Promethazine-d₆ (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is an orally active histamine receptor antagonist[1][2].

HY-114025

H4 Receptor antagonist 1	Histamine Receptor	Neurological Disease Endocrinology
H4 Receptor antagonist 1 is a potent and selective **histamine H4 receptor** inverse agonist, with an IC₅₀ of 19 nM.

HY-16756

Toreforant JNJ-38518168	Histamine Receptor	Neurological Disease Endocrinology
Toreforant is a potent and selective histamine H₄ receptor (H4R) antagonist, with a K_i at the human receptor of 8.4 nM.

HY-111501

H4R antagonist 1	Histamine Receptor	Inflammation/Immunology Endocrinology
H4R antagonist 1 is a potent and highly selective **histamine H4 receptor (H4R*) antagonist* with an IC₅₀ of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R .

HY-19048

CP-66948	Histamine Receptor	Endocrinology
CP-66948 is a **histamine H2-receptor** antagonist with gastric antisecretory activity and mucosal protective properties.

HY-B1510

Acrivastine BW825C	Histamine Receptor	Inflammation/Immunology Endocrinology
Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.

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-19580

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

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-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-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-17610

Enerisant TS-091	Histamine Receptor	Neurological Disease
Enerisant is a potent, highly selective, competitive and orally active **histamine H₃ receptor** antagonist/inverse agonist with IC₅₀s of 2.89 nM and 14.5 nM against human and rat histamine H₃ receptors, respectively .

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-B1510S

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

HY-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-107559

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

HY-115447

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

HY-B0377

Famotidine 4 Publications Verification MK-208	Histamine Receptor	Metabolic Disease Endocrinology Cancer
Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.

Cat. No.	Product Name	Type

HY-B0377G

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

Cat. No.	Product Name	Type

HY-B0377G

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

Cat. No.	Product Name	Target	Research Area

HY-P10619

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

HY-P3317

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

Cat. No.	Product Name	Category	Target	Chemical Structure

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-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-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-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-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-117500

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

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-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-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-107566

Conessine	Infection Structural Classification other families Classification of Application Fields Source classification Plants Disease Research Fields Steroids	Histamine Receptor Parasite
Conessine, a steroidal alkaloid, is a potent and selective **histamine H₃ receptor** antagonist with K_is of 5.4, 6.0, 5.7 and 25 nM for human, dog, guinea pig, and rat H H₃ receptor, respectively. Anti-malarial activity .

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-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-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-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-B0539

Desloratadine Maximum Cited Publications 9 Publications Verification Sch34117	Structural Classification Natural Products Classification of Application Fields Endogenous metabolite Disease Research Fields Endocrinology	Histamine Receptor TNF Receptor Leukotriene Receptor
Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (K_i=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria .

Cat. No.	Product Name	Chemical Structure

HY-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-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-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-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-B1296S

Promethazine-d6 hydrochloride
Promethazine-d₆ (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is an orally active histamine receptor antagonist[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-B1510S

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

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-19489S1

(Rac)-Levomepromazine-d3 hydrochloride
(Rac)-Levomepromazine-d₃ (hydrochloride) is a labelled racemic Methotrimeprazine, which is a phenothiazine which has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors[1][2].

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-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-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-B0377S

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

HY-A0077S2

Perphenazine-d6 fumarate

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

HY-B0160S

Lafutidine-d10
Lafutidine-d₁₀ is deuterium labeled Lafutidine. Lafutidine (FRG-8813) is a histamine H2-receptor antagonist (H2RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease[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][2][3].

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 .

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-B0274AS

Chlorprothixene-d6 hydrochloride
Chlorprothixene-d₆ (hydrochloride) is the deuterium labeled Chlorprothixene hydrochloride. Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity[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-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-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-B0281AS

Ranitidine-d6 hydrochloride
Ranitidine-d₆ (hydrochloride) is the deuterium labeled Ranitidine hydrochloride. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9[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-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-14289S

Cimetidine-d3
Cimetidine-d₃ is the deuterium labeled Cimetidine. Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity[1][2][5].

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-10121S2

Asenapine-13C,d3

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

HY-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-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-B0310S

Nizatidine-d3
Nizatidine-d₃ is the deuterium labeled Nizatidine. Nizatidine is a potent and orally active histamine H2 receptor antagonist, can be used for the research of stomach and intestines ulcers. Nizatidine works by decreasing the secretion of gastric acid the stomach makes and prevent ulcers from coming back after they have healed in animal models[1].

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-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-B0520AS1

Benztropine-d3 mesylate

Benztropine-d₃ (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2][3].

HY-B0520AS

Benztropine-13C,d3 mesylate

Benztropine- ¹³C,d₃ (mesylate) is the ¹³C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].

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].

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