The histamine H3-receptor: pharmacology, roles and clinical implications studied with agonists.
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.
Arrang
J M
JM
Unité de Neurobiologie et Pharmacologie, de l'INSERM, Centre Paul Broca, Paris, France.
Garbarg
M
M
Schwartz
J C
JC
Lipp
R
R
Stark
H
H
Schunack
W
W
Lecomte
J M
JM
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
D008761:Methylhistamines; D011968:Receptors, Histamine; D018100:Receptors, Histamine H3; D006632:Histamine