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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Bibliographic Details
Main Authors CARR ALBERT A, KOSLEY RAYMOND W. JR, VAN HIJFTE LUC E
Format Patent
LanguageEnglish
Polish
Published 31.01.2007
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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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.
Bibliography:Application Number: PL19980347318