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首页> 外文期刊>Pharmaceutical Chemistry Journal >SYNTHESIS AND ANALGESIC PROPERTIES OF NEW MODIFIED ANALOGS OF PHENCYCLIDINE WITH SPECIFIC BINDING ON PCP RECEPTOR OR DOPAMINE INHIBITION REUPTAKE ACTIVITIES
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SYNTHESIS AND ANALGESIC PROPERTIES OF NEW MODIFIED ANALOGS OF PHENCYCLIDINE WITH SPECIFIC BINDING ON PCP RECEPTOR OR DOPAMINE INHIBITION REUPTAKE ACTIVITIES

机译:在PCP受体或多巴胺抑制再摄取活性上特殊结合的新修饰酚类化合物类似物的合成与镇痛作用。

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Phencyclidine (PCP, I) and many of its analogs have showed many pharmacological effects through several neurotransmitter systems. In addition to binding to the N-methyl-d-aspartate (NMDA) subtype of the glutamate receptor, it also interferes with other brain functions. In this study, new derivatives (V - VII) were synthesized by changing aromatic moiety (phenyl, thienyl, and benzothiophene) and modifying cyclohexyl and piperidine rings (4-methylcyclohexyl and 3-piperidinol, respectively) of PCP. The acute and chronic pain activities of these new drugs were studied by using the tail immersion and formalin tests on mice and compared to control, PCP, and ketamine treated groups. The obtained results indicated that all new synthesized drugs showed better activity in decreasing acute thermal and chemical pains in tail immersion and formalin tests compared to PCP and ketamine. Also, compound VII (benzothiophene analog) produced more pronounced analgesic effects on acute thermal pain in tail immersion test, as well as compound V (thiophene analog) on acute chemical and chronic pains in formalin test as compared to other drugs.
机译:苯环利定(PCP,I)及其许多类似物通过几种神经递质系统表现出许多药理作用。除了与谷氨酸受体的N-甲基-d-天冬氨酸(NMDA)亚型结合外,它还干扰其他脑功能。在这项研究中,通过改变PCP的芳族部分(苯基,噻吩基和苯并噻吩)并修饰环己基和哌啶环(分别为4-甲基环己基和3-哌啶醇)来合成新的衍生物(V-VII)。通过在小鼠上进行尾部浸入和福尔马林测试,研究了这些新药的急性和慢性疼痛活性,并与对照组,PCP和氯胺酮治疗组进行了比较。所得结果表明,与PCP和氯胺酮相比,所有新合成药物在减少尾部浸入和福尔马林试验中的急性热和化学疼痛方面均显示出更好的活性。而且,与其他药物相比,化合物VII(苯并噻吩类似物)在尾部浸入试验中对急性热痛产生了更明显的镇痛作用,而化合物V(噻吩类似物)在福尔马林试验中对急性化学和慢性疼痛产生了更明显的镇痛作用。

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