[The histamine H(3) receptor: a target for new drugs].
The histamine H3 receptor has been identified in the rat brain as a presynaptic autoreceptor inhibiting histamine synthesis and release. Following its recent cloning, more than fifteen years later, the existence of isoforms, species pharmacological differences and the high constitutive activity of the receptor were established. All these molecular findings have to be taken into account for the optimization of the ligands aiming at a clinical use. They show the interest of antagonists/inverse agonists in the symptomatic treatment of schizophrenia and cognitive and attentional deficits.
Arrang
J-M
JM
Unité de neurobiologie et pharmacologie moléculaire, INSERM U573, Centre Paul Broca, 2ter, rue d'Alésia, F 75014 Paris.
D000818:Animals; D017660:Autoreceptors / Q000187:drug effects*; D017442:Histamine Agonists / Q000494:pharmacology* / Q000627:therapeutic use; D006633:Histamine Antagonists / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D051381:Rats; D018100:Receptors, Histamine H3 / Q000187:drug effects*
D017660:Autoreceptors; D017442:Histamine Agonists; D006633:Histamine Antagonists; D018100:Receptors, Histamine H3
Le récepteur H3 de l'histamine: une cible pour de nouveaux médicaments.