Histamine Receptor Agonist

Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

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.

Betazole hydrochloride (Ametazole hydrochloride), 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.

MK-3134 is an orally active, brain-penetrant and selective histamine H3 receptor inverse agonist. MK-3134 modulates histaminergic neurotransmission, decreases constitutive H3 receptor signaling, releases tonic inhibition of neurotransmitter release, potentiates neurotransmission, and may enhance cholinergic neurotransmission. MK-3134 can be used for the research of Alzheimer's disease.

Histamine dihydrochloride is the agonist for histamine receptor and a vasodilator. Histamine dihydrochloride is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine dihydrochloride affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

Histamine phosphate is the agonist for histamine receptor and a vasodilator. Histamine phosphate is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine phosphate affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine phosphate can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

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) .

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 .

N-Methylhistamine dihydrochloride (Nα-Methylhistamine dihydrochloride) is a non-selective Histamine receptor agonist. N-Methylhistamine dihydrochloride activates histamine H₁, H₂ and H₃ receptors; it stimulates central H₁ receptors by activating sympathetic α and β adrenergic receptors to inhibit intestinal transit, exerts dose-dependent inhibition on intestinal transit, reduces histamine turnover in mouse brains, and increases gastric acid secretion without altering plasma gastrin concentrations. N-Methylhistamine dihydrochloride produces a pH-dependent, voltage-independent potentiating effect on acid-sensing ion channel 1a, and shows no significant activity toward homologous ASIC2a channels. N-Methylhistamine dihydrochloride can be used in studies related to Helicobacter pylori infection.

4-Methylhistamine hydrochloride is the dihydrochloride salt of 4-Methylhistamine (HY-W580721). 4-Methylhistamine hydrochloride is a potent and selective agonist of histamine 4 receptor (H4R) with a K_i of 50 nM. 4-Methylhistamine hydrochloride has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine hydrochloride can potently activate the hH4R (pEC₅₀ = 7.4). 4-Methylhistamine hydrochloride can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation.

Histamine (Standard) is the analytical standard of Histamine (HY-B1204). This product is intended for research and analytical applications. Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

(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.

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.

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).

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

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.

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.

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.

Histamine dihydrochloride (Standard) is the analytical standard of Histamine dihydrochloride (HY-B0722). This product is intended for research and analytical applications. Histamine dihydrochloride is the agonist for histamine receptor and a vasodilator. Histamine dihydrochloride is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine dihydrochloride affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

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.