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The histamine H3-receptor: pharmacology, roles and clinical implications studied with agonists
J M Arrang1, M Garbarg, J C Schwartz
1Unité de Neurobiologie et Pharmacologie, de l'INSERM, Centre Paul Broca, Paris, France.
Agents and Actions. Supplements
|January 1, 1991
Abstract:
Among a series of methylated histamine derivatives, (R) alpha, (S) beta,-dimethylhistamine has been identified as a novel potent and selective H3-receptor agonist, even slightly more potent than (R) alpha-methylhistamine and displaying similar properties in vivo. Several studies suggesting that (R) alpha-methylhistamine might find various clinical applications, it was submitted to toxicological studies and initial clinical trials. The drug seems to display a very low animal toxicity, and, in humans, is well absorbed orally and metabolized via ring methylation before urinary excretion.