Ahmadi Abbas, Khalili Mohsen, Mihandoust Farnaz, Barghi Leila
Department of Chemistry, Faculty of Sciences, Islamic Azad University, Karaj Branch, Karaj, Iran.
Arzneimittelforschung. 2010;60(1):30-5. doi: 10.1055/s-0031-1296245.
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.
苯环己哌啶（1-（1-苯基环己基）哌啶，CAS 956-90-1，PCP，1）和氯胺酮（2-O-氯苯基-2-甲基氨基环己烷，CAS 1867-66-9，II）显示出一些镇痛作用。已合成它们的一些衍生物用于生物学特性研究。以1-四氢萘酮为起始原料，合成了1-[1-（3-甲基苯基）（四氢萘基）]哌啶（PCP-CH3-四氢萘基，III），并通过尾浸法（作为急性热痛模型）和福尔马林（作为急性化学性和慢性疼痛模型）试验研究了其对大鼠的镇痛作用，并与氯胺酮和PCP的镇痛作用进行了比较。结果表明，氯胺酮注射后2-25分钟有明显的抗伤害感受作用，但在尾浸试验中应用PCP-CH3-四氢萘基后，这种镇痛作用持续40分钟。然而，从福尔马林试验获得的数据表明，氯胺酮、PCP和PCP-CH3-四氢萘基可显著减轻慢性疼痛。
