Drug intelligence / Profile preview

r(-)-alpha-methyl-histamine

Development stage
Preclinical
Modality
Small Molecules
Administration
Experimental (systemic, I.g. In Animal Models)
01

Overview

(R)-alpha-methylhistamine is a synthetic, chiral, small molecule that acts as a potent and selective agonist for the **histamine H3 receptor**. Its (R)-enantiomer shows much higher activity than the (S)-enantiomer. The compound is mainly utilized as a pharmacological tool in research to study histamine H3 receptor pathways, including neuronal histamine release, gastric acid secretion modulation, and gastroprotective processes. It demonstrates high affinity with a \( K_i \) in the nanomolar range and exhibits over 200-fold selectivity for H3 over other histamine receptors[11][7][20][1][18][19]. Research applications have included investigations into gastrointestinal physiology, CNS function, and immunological responses. The molecule is for research use only and not approved for therapeutic use. Developers and manufacturers supply this compound as dihydrochloride and dihydrobromide salts for laboratory and pharmacological studies.

Other names
(R)-alpha-methylhistamine(R)(−)-α-Methylhistamine(R)-(-)-α-Methylhistamine(R)-alpha-methyl-1H-imidazole-4-ethanamine(2R)-1-(1H-imidazol-5-yl)propan-2-amine
02

Targets

HRH3 (Histamine Receptor H3)

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