R(-)-α-Methylhistamine·2HBr (CAS 75614-87-8)

R(-)-α-Methylhistamine·2HBr is a small molecule agonist of the histamine H₃-receptor, with at least one order of magnitude higher affinity for the H₃-receptor than histamine itself. The H₃-receptor is responsible for feedback control of histamine secretion and release from cerebral histaminergic neurons, and agonism of this receptor by R(-)-α-Methylhistamine·2HBr has been used to elucidate the feedback mechanism. Inhibition of histamine synthesis in response to depolarising stimuli is induced by histamine-H₃-receptor association, and this effect is mimicked by R(-)-α-Methylhistamine·2HBr agonism. The release of histamine is also attenuated by stimulation of the H₃-receptor, and agonism by R(-)-α-Methylhistamine·2HBr mimics this endogenous function of histamine as well. Agonism of the H₃-receptor by R(-)-α-Methylhistamine·2HBr is described to inhibit cholinergic neurotransmission and subdue contractile response of longitudinal ileum smooth muscle to electrically-stimulated acetylcholine release.

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