title: The histamine H3-receptor: pharmacology, roles and clinical implications studied with agonists.
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.
authors.affiliation: Unité de Neurobiologie et Pharmacologie, de l'INSERM, Centre Paul Broca, Paris, France.
authors.forename: J M
authors.initials: JM
authors.lastname: Arrang
authors.forename: M
authors.initials: M
authors.lastname: Garbarg
authors.forename: J C
authors.initials: JC
authors.lastname: Schwartz
authors.forename: R
authors.initials: R
authors.lastname: Lipp
authors.forename: H
authors.initials: H
authors.lastname: Stark
authors.forename: W
authors.initials: W
authors.lastname: Schunack
authors.forename: J M
authors.initials: JM
authors.lastname: Lecomte
mesh_terms: D000818:Animals; D006632:Histamine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D008761:Methylhistamines / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D011968:Receptors, Histamine / Q000187:drug effects / Q000502:physiology*; D018100:Receptors, Histamine H3
chemical_list: D008761:Methylhistamines; D011968:Receptors, Histamine; D018100:Receptors, Histamine H3; D006632:Histamine