Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?
A new diaryl-methylene piperidine derivative, 2, displayed an atypical antipsychotic profile both in vitro and in vivo. The main pharmacological characteristics of this compound appears to reside in a more potent antagonism of the 5-HT2 serotonergic receptor than of the D2 dopaminergic receptor. This confirms that molecules displaying a D2/5-HT2 binding ratio < 1 possess clozapine-like antipsychotic activity.
Talaga
P
P
UCB SA, Pharma Sector, Chemin du Foriest, Braine-l'Alleud, Belgium. patrice.talaga@ucb-group.com
Matagne
A
A
Klitgaard
H
H
D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology / Q000633:toxicity; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D051379:Mice; D010880:Piperidines / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D011485:Protein Binding; D011595:Psychomotor Agitation / Q000188:drug therapy; D011618:Psychotic Disorders / Q000188:drug therapy; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology / Q000633:toxicity
D014150:Antipsychotic Agents; D010880:Piperidines; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists