Histamine Receptor Agonist

Immethridine (dihydrobromide) is a potent and highly selective histamine H₃ receptor agonist with pK_i and pEC₅₀ value of 9.07 and 9.74, respectively. Immethridine can be used for the research of myocardial ischemia, inflammatory, and gastric acid related diseases research.

(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.

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.

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

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.

4-Methylhistamine hydrochloride is the hydrochloride 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.

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.

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.

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.

VUF14480 is a partial agonist of histamine H4 (hH4) receptor-mediated G protein signalling and β-arrestin2 recruitment. VUF14480 binds covalently to hH4 receptor (pK_i: 6.3 for hH4-WT receptor). VUF14480 partially induces hH4 receptor-mediated G protein activation and β-arrestin2 recruitment. VUF14480 can be used in the research of inflammatory diseases.

8 Hydroxy PIPAT oxalate is a 5-HT_1A receptor agonist that promotes histamine release. 8 Hydroxy PIPAT oxalate selectively activates 5-HT_1A receptors, thereby triggering mast cell degranulation and histamine release. 8 Hydroxy PIPAT oxalate is applicable to research related to irritable bowel syndrome.

Methimepip dihydrobromide is a potent and selective histamine H3 receptor agonist with an EC₅₀ of 0.316nM.

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.

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

Histamine phosphate (Standard) is the analytical standard of Histamine phosphate (HY-A0129). This product is intended for research and analytical applications. 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.

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.

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.

VUF5207, an Impentamine (HY-107564) analogue, is a partial agonist of histamine H3 receptor.

H3R antagonist 5 (Compound 1b) is a selective histamine H3 receptor inverse agonist with a IC₅₀ of 0.54 nM and the ability to cross the blood-brain barrier. H3R antagonist 5 can be used in central nervous system-related research.