Clozapine is a partial agonist at cloned, human serotonin 5-HT1A receptors.
Clozapine exhibited 10-fold higher affinity than haloperidol for human 5-HT1A receptors expressed in Chinese Hamster Ovary cells (CHO-h5-HT1A) (Kis = 160 and 1910 nM respectively). Whereas haloperidol did not alter the basal binding of [35S]GTP gama S to CHO-h5HT1A membranes, clozapine stimulated it with an EC50 of 2320 nM and an efficacy of 49% (compared to 5-HT). The stimulation was antagonized by the selective 5-HT1A receptor antagonist, WAY 100635 (1 nM).
Newman-Tancredi
A
A
Department of Psychopharmacology, Institut de Recherches Servier, Croissy-sur-seine, Paris, France.
Chaput
C
C
Verriele
L
L
Millan
M J
MJ
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive; D016466:CHO Cells; D003024:Clozapine / Q000494:pharmacology*; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D006220:Haloperidol / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D011985:Receptors, Serotonin / Q000187:drug effects*
D011985:Receptors, Serotonin; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D003024:Clozapine; D006220:Haloperidol