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
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 : Neu...
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Main Authors | , , |
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Format | Patent |
Language | English Polish |
Published |
31.01.2007
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Subjects | |
Online Access | Get full text |
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Summary: | 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. |
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Bibliography: | Application Number: PL19980347318 |