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.
Ahmadi
Abbas
A
Department of Chemistry, Faculty of Sciences, Islamic Azad University, Karaj Branch, Karaj, Iran. abbas_ahmady_3957@yahoo.com
Khalili
Mohsen
M
Mihandoust
Farnaz
F
Barghi
Leila
L
D000208:Acute Disease; D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000778:Anesthetics, Dissociative / Q000494:pharmacology; D000818:Animals; D002908:Chronic Disease; D005260:Female; D005557:Formaldehyde; D007101:Immersion; D007649:Ketamine / Q000494:pharmacology; D010147:Pain Measurement / Q000187:drug effects*; D010622:Phencyclidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar
D000700:Analgesics; D000778:Anesthetics, Dissociative; D005557:Formaldehyde; D007649:Ketamine; D010622:Phencyclidine