Synthesis and Study the Analgesic Effects of New Analogues of Ketamine on Female Wistar Rats
Synthesis and Study the Analgesic Effects of New Analogues of Ketamine on Female Wistar Rats
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DOI：
10.2174/157340612800493683
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发表时间：
2012-03-01
影响因子：
2.3
通讯作者：
Nahri-Niknafs, Babak
中科院分区：
文献类型：
--
作者：
Ahmadi, Abbas;Khalili, Mohsen;Nahri-Niknafs, Babak
氯胺酮（2-邻氯苯基-2-甲基氨基环己烷，CAS 1867-66-9，CI-581，氯胺酮，I）是苯环己哌啶（1-[1-苯基环己基]哌啶，CAS 956-90-1，PCP，II）的强效衍生物，其许多类似物已显示出麻醉和镇痛作用。在这项研究中，新的衍生物的I，（2-[对甲氧基苄基氨基]-2-[对甲氧基苯基]环己酮，ket-OCH 3，III），（2-[对甲基苄基氨基]-2-[对甲氧基苯基]环己酮，酮-CH 3，IV）及其中间体（V-VIII）的合成，并采用大鼠浸泡法对III和IV的急性和慢性疼痛进行了评价（作为急性热疼痛的模型）和福尔马林（作为急性和慢性化学疼痛的模型）测试。并与氯胺酮组和生理盐水对照组进行比较。结果表明，在尾部浸泡和福尔马林试验中，这些新的衍生物（III和IV）通常对减轻大鼠疼痛有效。
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.