Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj branch, Karaj, Iran.
Med Chem. 2012 Mar;8(2):246-51. doi: 10.2174/157340612800493683.
Ketamine (2-o-chlorophenyl-2-methylaminocyclohexan, CAS 1867-66-9, CI-581, Ketalar, I), a potent derivative of Phencyclidine (1-[1-phenylcyclohexyl] piperidine, CAS 956-90-1, PCP, II), and many of its analogues have shown anesthetic and analgesic effects. In this research, new derivatives of I, (2-[p-methoxybenzylamino]-2-[p-methoxyphenyl] cyclohexanone, ket-OCH3, III), (2-[p-methylbenzylamino]-2-[p-methoxyphenyl] cyclohexanone, ket-CH3, IV) and their intermediates (V-VIIII) were synthesized and the acute and chronic pains of III and IV were evaluated on rats using tail immersion (as a model of acute thermal pain) and formalin (as a model of acute and chronic chemical pain) tests. The results werecompared with ketamine and control (saline) groups. The results indicated that in tail immersion and formalin tests, these new derivatives (III and IV) were usually effective for decreasing pain on rats.
氯胺酮（2-邻氯苯基-2-甲基氨基环己酮，CAS 1867-66-9，CI-581，Ketalar，I）是苯环己哌啶（1-[1-苯基环己基]哌啶，CAS 956-90-1，PCP，II）的一种强效衍生物，以及许多类似物已显示出麻醉和镇痛作用。在这项研究中，I 的新衍生物（2-[对甲氧基苄基氨基]-2-[对甲氧基苯基]环己酮，酮-OCH3，III），（2-[对甲基苄基氨基]-2-[对甲氧基苯基]环己酮，酮-CH3，IV）及其中间体（V-VIII）被合成，并使用尾巴浸泡（作为急性热痛模型）和福马林（作为急性和慢性化学痛模型）测试在大鼠上评估 III 和 IV 的急性和慢性疼痛。结果与氯胺酮和对照组（生理盐水）进行了比较。结果表明，在尾巴浸泡和福马林测试中，这些新衍生物（III 和 IV）通常可有效减轻大鼠的疼痛。
