Synthesis and determination of acute and chronic pain activities of 1-[1-(3-methylphenyl) (tetralyl)]piperidine as a new derivative of phencyclidine via tail immersion and formalin tests.

Phencyclidine (1-(1-phenylcyclohexyl)piperidine, CAS 956-90-1, PCP, 1) and ketamine (2-O-chlorophenyl-2-methylaminocyclohexan, CAS 1867-66-9, II) revealed some analgesic effects. Some of their derivatives have been synthesized for biological properties studies. Utilizing 1-tetralone as a starting material, 1-[1-(3-methylphenyl)(tetralyl)]piperidine, (PCP-CH3-tetralyl, III) was synthesized and its analgesic effects were studied on rats via tail immersion (as a model of acute thermal pain) and formalin (as a model of acute chemical and chronic pain) tests and compared with those of ketamine and PCP. The results indicated a marked anti-nociception 2-25 min after ketamine injection, but this analgesic effect lasted for 40 min following PCP-CH3-tetralyl application in the tail immersion test. However, the data obtained from the formalin test showed that chronic pain could be significantly attenuated by ketamine, PCP and PCP-CH3-tetralyl.

Synthesis and determination of chronic and acute thermal and chemical pain activities of a new derivative of phencyclidine in rats.

Phencyclidine (1-(1-phenylcyclohexyl) piperidine, PCP, I) and ketamine (2-O-chlorophenyl-2-methylaminocyclohexan, II) have shown analgesic effects. Some of its derivatives were synthesized and their biological properties have been studied. In this study, a new derivative of PCP, (1-[1-(3-methoxyphenyl) (tetralyl)] piperidine, PCP-OCH3-tetralyl, III) was synthesized and the acute thermal pain of this compound was determined using tail immersion test on rats and the results were compared with Ketamine and PCP. The results indicated a marked anti-nociception 2-25 min after ketamine injection, but the analgesic effect remained for 40 min following PCP-OCH3-tetralyl application in tail immersion test. However, the data obtained from formalin test showed that the chronic anti-nociception effect of ketamine was higher than PCP and PCP-OCH3-tetralyl exhibited almost similar analgesic effect.