Histamine Receptor Agonist

Histamine Receptor Agonists (46):

Cat. No.	Product Name	Effect	Purity

HY-17043

Loratadine	Agonist	99.98%
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-A0129

Histamine phosphate	Agonist	99.99%
Histamine (phosphate) is a strong histamine receptor activator and vasodilator neuroagent, capable of activating nitric oxide synthase.

HY-107560

4-Methylhistamine dihydrochloride	Agonist	99.35%
4-Methylhistamine (dihydrochloride) is the potent agonist of histamine 4 receptor (H4R). 4-Methylhistamine (dihydrochloride) has the potential for the research of immune-related diseases such as cancer and autoimmune disorders.

HY-101063

Amthamine dihydrobromide	Agonist	99.64%
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-B1557

Betazole	Agonist
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-W014941

(R)-(-)-α-Methylhistamine dihydrochloride	Agonist	99.62%
(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a K_d of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats.

HY-B1478

Dimaprit dihydrochloride	Agonist	99.91%
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-107565

2-Pyridylethylamine hydrochloride	Agonist	99.86%
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-101420

VUF10460	Agonist	99.28%
VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pK_i of 7.46.

HY-12752A

Alimemazine hemitartrate	Agonist	98.44%
Alimemazine hemitartrate (Trimeprazine hemitartrate) is an antagonist of the histamine (HA) receptor that can be taken orally and also acts as a partial agonist at other GPCR receptors. Alimemazine hemitartrate has effects that include anti-serotonin, antispasmodic, antihistamine, sedation, hypnotic, antiviral, and anti-nausea properties. Alimemazine hemitartrate promotes the growth of pancreatic β-cells in mice and improves diabetes in mice.

HY-128656

LML134	Agonist	99.43%
LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with K_is of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders.

HY-120541

ST-1006	Agonist	99.55%
ST-1006 is a potent histamine H4 receptor agonist with a pK_i value of 7.94. ST-1006 has anti-inflammatory effect.

HY-101173

Imetit dihydrobromide	Agonist	≥98.0%
Imetit dihydrobromide (VUF 8325 dihydrobromide) is a high affinity and potent agonist of histamine H3 and H4 receptors, with K_i values of 0.3 and 2.7 nM, respectively. Imetit mimics histamine effect in triggering a shape change in eosinophils (EC₅₀=25 nM).

HY-100999

(R)-(-)-α-Methylhistamine dihydrobromide	Agonist
(R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a K_d of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrobromide can enhance memory retention, attenuates memory impairment in rats.

HY-101052

HTMT dimaleate	Agonist	99.55%
HTMT (dimaleate) is a potent histamine H1 and H2 receptor agonist. HTMT (dimaleate) is 4 x 10⁴ times more active than histamine in H2-mediated effects in natural suppressor cells.

HY-W580721A

4-Methylhistamine hydrochloride	Agonist
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-122608

Samelisant free base	Agonist
Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; K_i=8.7 nM) and rat (rH3R;K_i=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders.

HY-17043S

Loratadine-d₄	Agonist
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-108058A

Immethridine dihydrobromide	Agonist
Immethridine dihydrobromide is a selective histamine H3 receptor (H3R) agonist. Immethridine dihydrobromide displays 300-fold selectivity over the H4 receptor and does not bind to H1 or H2 receptors. Immethridine dihydrobromide can be used for experimental autoimmune encephalomyelitis (EAE) research.

HY-B0377G

Famotidine (GMP)	Agonist
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.

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