PHARMACOLOGICAL STUDIES OF 1-PHENACYL-2, 3-DIMETHYL-3-(3-HYDROXYPHENYL) PIPERIDINE HYDROCHLORIDE (TA-306), AN ANALGESIC AND ANTITUSSIVE AGENT

Abstract

Many analogs of iso-pethidine have been synthesized and examined for their analgesic activities, which, however were found lower than those of meperidine (1, 2). The authors, studying pharmacological effects of N-transferred compounds of benzomorphan (3), found that some of 3-phenyl-piperidine derivatives possessed strong analgesic effectiveness, and investigated the relationship between chemical structures and biological activities (4, 5). Among them 1-phenacyl-2, 3-dimethyl-3-(3-hydroxyphenyl) piperidine hydrochloride (TA-306) showed the most potent analgesic effect and low toxicity. The compound did not suppress abstinence signs of the monkey physically dependent on morphine (6). In this report are described further studies of the analgesic activity of TA-306 and comparative pharmacological studies of the drug with morphine hydrochloride and meperidine hydrochloride.