ESTERS OF (+)-ALPHA-(2,3-DIMETHOXYPHENYL)-1-[2-(4-FLUOROPHENYL)ETHYL]-4-PIPERIDINEMETHANOL AND THEIR USE AS PRODRUGS OF THE 5HT2A RECEPTOR ANTAGONIST MDL 110,907

摘要

Esters of (2,3-dimethoxy-phenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol (MDL 100907) (I), are new. Esters of (+)-alpha-(2,3-dimethoxy- phenyl)-1-[2(4-fluorophenyl)ethyl]-4-piperidine methanol of formula (I) and their stereoisomers and salts are new. [Image] R : 4-20C alkyl. ACTIVITY : Neuroleptic; Antimanic; Antidepressant; Tranquilizer; Antiaddictive; Cardiant; Antianginal; Thrombolytic; Eating-Disorders-Gen.; Vasotropic; Antiarrhythmic; Sedative. (+)-alpha-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl(ethyl]-4- piperidine methanol decanoate (120 mg/kg equivalent to MDL-100907) was administered to (+/-)-DOI HCl injected male Sprague-Dawley rats. (+/-)-DOI HCl induces several quantifiable behaviours in rats. Significantly antagonized DOI-induced behavior in the rats was observed for a full 28 days. The effect was no longer significant at day 40. MECHANISM OF ACTION : Antiserotonin-2A.