Synthesis and metabolic profile of Cl-966: A potent, orally-active inhibitor of GABA uptake

Autor:	Louis L. Radulovic, Ann E. Black, Tsun Chang, Susan M. Bjorge, Michael R. Pavia, Thomas F. Woolf, Sandra J. Lobbestael, David Nugiel, Vlad E. Gregor, Howard N. Bockbrader
Rok vydání:	1990
Předmět:	chemistry.chemical_classification chemistry.chemical_compound Guvacine Trifluoromethyl chemistry Stereochemistry Oral administration Carboxylic acid Metabolite Drug Discovery Pyridinium Metabolism Chemical synthesis
Zdroj:	Drug Development Research. 21:189-193
ISSN:	1098-2299 0272-4391
DOI:	10.1002/ddr.430210305
Popis:	A lipophilic derivative of the known GABA uptake inhibitor guvacine has been prepared. The synthesis of this compound, [1-]2-bis 4-(trifluoromethyl)]phenyl[-methoxy]ethyl[- 1,2,5,6-tet-rahydro-3-pyridine carboxylic acid, monohydrochloride, Cl-966, is described. Studies were carried out to determine the metabolic profile of Cl-966, in rats. Two metabolites, one less polar and the other more polar than Cl-966, were identified and their structures assigned by spectroscopic methods and confirmed by comparison to synthetic material.
Databáze:	OpenAIRE
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