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histamine receptors-agonists

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Histamine Receptor (35) 5-HT Receptor (9) Adenosine Receptor (1) Adrenergic Receptor (5) Dengue virus (3) Flavivirus (3) Isotope-Labeled Compounds (5) mAChR (5) NO Synthase (1) Serotonin Transporter (5) Sodium Channel (5) Trk Receptor (5)
By Research Areas:	Cancer (7) Endocrinology (11) Infection (5) Inflammation/Immunology (21) Metabolic Disease (3) Neurological Disease (18)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: Histamine Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-101063

Amthamine dihydrobromide	Histamine Receptor	Inflammation/Immunology
Amthamine is a histamine receptor (H1R-H4R) agonist. Amthamine can produce liver congestion and necrosis of liver cells. Amthamine can be used to study the induction effect of H1R-H4 agonist on hepatotoxicity .

HY-107555

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

HY-101420

VUF10460	Histamine Receptor	Inflammation/Immunology Endocrinology
VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pK_i of 7.46.

HY-101052

HTMT dimaleate	Histamine Receptor	Inflammation/Immunology
HTMT (dimaleate) is a potent **histamine H1 and H2 receptor** agonist. HTMT (dimaleate) is 4 x 10 ⁴ times more active than histamine in H2-mediated effects in natural suppressor cells .

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-B1478

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

HY-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-129508

Amthamine	Histamine Receptor	Inflammation/Immunology
Amthamine is a histamine receptor (H1R-H4R) agonist. Amthamine can produce liver congestion and necrosis of liver cells. Amthamine can be used to study the induction effect of H1R-H4 agonist on hepatotoxicity .

HY-108977

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

HY-107565

2-Pyridylethylamine hydrochloride	Histamine Receptor	Inflammation/Immunology
2-Pyridylethylamine is a histamine-1 (H1R) receptor agonist. 2-Pyridylethylamine can reduce the joint injury induced by formalin in rats. 2-Pyridylethylamine can be used to study the spinal cord release of neuropeptide (NPY) .

HY-120541A

ST-1006 Maleate	Histamine Receptor	Inflammation/Immunology
ST-1006 maleate is a potent **histamine H4 receptor** agonist with a pK_i value of 7.94. ST-1006 maleate has anti-inflammatory effect .

HY-120541

ST-1006	Histamine Receptor	Inflammation/Immunology
ST-1006 is a potent **histamine H4 receptor** agonist with a pK_i value of 7.94. ST-1006 has anti-inflammatory effect .

HY-B1557

Betazole 1 Publications Verification Ametazole	Histamine Receptor	Metabolic Disease
Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active **histamine H2 receptor** agonist. Betazole induces gastric acid secretion and causes an immediate and significant increase in common bile duct pressure. Betazole is used as a diagnostic agent known as histalog for investigating gastric acid secretory capacity .

HY-W580721A

4-Methylhistamine hydrochloride	Histamine Receptor	Others
4-Methylhistamine (hydrochloride) is a potent, high affinity H4 receptor agonist K_i of 7 nM. 4-Methylhistamine (hydrochloride) displays more than 100-fold selectivity over other human histamine receptor subtypes .

HY-19365

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

HY-B0524AS

Betahistine-d3 dihydrochloride	Histamine Receptor	Neurological Disease Inflammation/Immunology Endocrinology
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-B1557R

Betazole (Standard)	Histamine Receptor	Metabolic Disease
Betazole (Standard) is the analytical standard of Betazole. This product is intended for research and analytical applications. Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active **histamine H2 receptor** agonist. Betazole induces gastric acid secretion and causes an immediate and significant increase in common bile duct pressure. Betazole is used as a diagnostic agent known as histalog for investigating gastric acid secretory capacity .

HY-B0524AR

Betahistine (dihydrochloride) (Standard)	Histamine Receptor	Neurological Disease Inflammation/Immunology Endocrinology
Betahistine (dihydrochloride) (Standard) is the analytical standard of Betahistine (dihydrochloride). This product is intended for research and analytical applications. 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-D0237R

Betahistine (mesylate) (Standard)	Histamine Receptor	Inflammation/Immunology
Betahistine (mesylate) (Standard) is the analytical standard of Betahistine (mesylate). This product is intended for research and analytical applications. 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-17043

Loratadine Maximum Cited Publications 6 Publications Verification 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-107495

Betahistine EP Impurity C NSC19005	Histamine Receptor	Inflammation/Immunology
Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine . Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA) .

HY-113802

VUF 8328	Histamine Receptor	Neurological Disease
VUF 8328 is a potent **histamine H(3) receptor** agonist. VUF 8328 inhibits the electrically-evoked [ ³H]-no-radrenaline release from rat cortical slices. VUF 8328 is promising for research of central nervous system disorders .

HY-B0524AS1

Betahistine-13C,d3 dihydrochloride	Isotope-Labeled Compounds Histamine Receptor	Neurological Disease Inflammation/Immunology Endocrinology
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-17043S

Loratadine-d4 Loratidine-d₄; SCH 29851-d₄	Isotope-Labeled Compounds Histamine Receptor	Infection Inflammation/Immunology Endocrinology
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 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-B1557A

Betazole dihydrochloride Ametazole dihydrochloride	Histamine Receptor	Metabolic Disease
Betazole (Ametazole) dihydrochloride, a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole dihydrochloride induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole dihydrochloride has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity .

HY-17043R

Loratadine (Standard)	Dengue virus Flavivirus 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-101225

8 Hydroxy PIPAT oxalate	Histamine Receptor	Inflammation/Immunology
8 Hydroxy PIPAT oxalate is a selective 5-HT1A receptor agonist that promotes the release of histamine from enteric mast cells. 8 Hydroxy PIPAT oxalate activates serotonergic signaling pathways, leading to the degranulation of mast cells in both guinea pig and human intestinal preparations. 8 Hydroxy PIPAT oxalate enhances the spontaneous release of histamine, which may contribute to the regulation of gastrointestinal functions. 8 Hydroxy PIPAT oxalate has potential implications for understanding and treating functional gastrointestinal disorders such as irritable bowel syndrome.

HY-17043S2

Loratadine-d4-1 Loratidine-d₄-1; SCH 29851-d₄-1	Isotope-Labeled Compounds Histamine Receptor Dengue virus Flavivirus	Infection Inflammation/Immunology Endocrinology Cancer
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 .

HY-167897

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

HY-B0527A

Amitriptyline hydrochloride 4 Publications Verification	Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor	Neurological Disease Cancer
Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with K_is of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a K_i of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, *histamine* and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .

HY-B0527

Amitriptyline 4 Publications Verification	Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor	Neurological Disease Cancer
Amitriptyline is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with K_is of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline also weakly binds to dopamine reuptake transporter (DAT) with a K_i of 2.58 μM. Amitriptyline also inhibits adrenergic, muscarinic, *histamine* and 5-HT receptors. Amitriptyline is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline has antidepressant activity .

HY-B0527AS

Amitriptyline-d6 hydrochloride	Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor	Neurological Disease
Amitriptyline-d₆ (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].

HY-135096

Amitriptyline-d3 hydrochloride	Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor	Neurological Disease
Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with K_is of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a K_i of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, *histamine* and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .

HY-B0527AR

Amitriptyline (hydrochloride) (Standard) 4 Publications Verification	Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor	Neurological Disease Cancer
Amitriptyline (hydrochloride) (Standard) is the analytical standard of Amitriptyline (hydrochloride). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with K_is of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a K_i of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, *histamine* and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .

HY-B1658A

Frovatriptan succinate hydrate (R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrate	5-HT Receptor	Neurological Disease
Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT_1B (pK₅₀ of 8.2) and 5-HT_1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT_1B and 5-HT_1D over 5-HT_1A, 5-HT_1F, and 5-HT₇ and >1000-fold selectivity over other 5-HT, dopamine, histamine H₁, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research .

HY-B1658B

Frovatriptan succinate (R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate	5-HT Receptor	Neurological Disease
Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT_1B (pK₅₀ of 8.2) and 5-HT_1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT_1B and 5-HT_1D over 5-HT_1A, 5-HT_1F, 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 .

HY-B1658BS

Frovatriptan-d3 succinate (R)-Frovatriptan-d₃ succinate; SB 209509-d₃ succinate; VML 251-d₃ succinate	Isotope-Labeled Compounds 5-HT Receptor	Neurological Disease
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].

HY-B1658AR

Frovatriptan (succinate hydrate) (Standard)	5-HT Receptor	Neurological Disease
Frovatriptan (succinate hydrate) (Standard) is the analytical standard of Frovatriptan (succinate hydrate). This product is intended for research and analytical applications. Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate 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 hydrate has the potential for migraine research .

Cat. No.	Product Name	Chemical Structure

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-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-B0527AS

Amitriptyline-d6 hydrochloride
Amitriptyline-d₆ (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].

Amitriptyline-d6 hydrochloride

Amitriptyline-d₆ (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].

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-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-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 .

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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