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

Abstract

Abstract 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.