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.

Abstract

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.

• Authors: Abbas Ahmadi, Mohsen Khalili, Farnaz Mihandoust, Leila Barghi
• Journal: Arzneimittel-Forschung (Arzneimittelforschung) Vol. 60 Issue 1 Pg. 30-5 ( 2010) ISSN: 0004-4172 [Print] Germany
• PMID: 20184224 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Analgesics
• Anesthetics, Dissociative
• Formaldehyde
• Ketamine
• Phencyclidine

Topics

• Acute Disease
• Analgesics (chemical synthesis, chemistry, pharmacology)
• Anesthetics, Dissociative (pharmacology)
• Animals
• Chronic Disease
• Female
• Formaldehyde
• Immersion
• Ketamine (pharmacology)
• Pain Measurement (drug effects)
• Phencyclidine (analogs & derivatives, chemical synthesis, chemistry, pharmacology)
• Rats
• Rats, Wistar