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苯环己哌啶新衍生物在大鼠体内慢性和急性热痛及化学性疼痛活性的合成与测定

Synthesis and determination of chronic and acute thermal and chemical pain activities of a new derivative of phencyclidine in rats.

作者信息

Ahmadi Abbas, Khalili Mohsen, Hajikhani Ramin, Barghi Leila, Mihandoust Farnaz

机构信息

epartment of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran.

Department of Physiology, School of Medicine, Shahed University, Tehran, Iran.

出版信息

Iran J Pharm Res. 2010 Fall;9(4):379-85.

PMID:24381602
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3870061/
Abstract

Phencyclidine (1-(1-phenylcyclohexyl) piperidine, PCP, I) and ketamine (2-O-chlorophenyl-2-methylaminocyclohexan, II) have shown analgesic effects. Some of its derivatives were synthesized and their biological properties have been studied. In this study, a new derivative of PCP, (1-[1-(3-methoxyphenyl) (tetralyl)] piperidine, PCP-OCH3-tetralyl, III) was synthesized and the acute thermal pain of this compound was determined using tail immersion test on rats and the results were compared with Ketamine and PCP. The results indicated a marked anti-nociception 2-25 min after ketamine injection, but the analgesic effect remained for 40 min following PCP-OCH3-tetralyl application in tail immersion test. However, the data obtained from formalin test showed that the chronic anti-nociception effect of ketamine was higher than PCP and PCP-OCH3-tetralyl exhibited almost similar analgesic effect.

摘要

苯环己哌啶(1-(1-苯基环己基)哌啶,PCP,I)和氯胺酮(2-O-氯苯基-2-甲氨基环己烷,II)已显示出镇痛作用。合成了其一些衍生物并研究了它们的生物学特性。在本研究中,合成了一种新的PCP衍生物(1-[1-(3-甲氧基苯基)(四氢萘基)]哌啶,PCP-OCH3-四氢萘基,III),并使用大鼠尾部浸入试验测定了该化合物的急性热痛,并将结果与氯胺酮和PCP进行比较。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,但在尾部浸入试验中应用PCP-OCH3-四氢萘基后镇痛作用持续40分钟。然而,从福尔马林试验获得的数据表明,氯胺酮的慢性抗伤害感受作用高于PCP,且PCP-OCH3-四氢萘基表现出几乎相似的镇痛作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41c6/3870061/339884d83eed/ijpr-09-379-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41c6/3870061/289be1d4646d/ijpr-09-379-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41c6/3870061/7bfaec7ae4e7/ijpr-09-379-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41c6/3870061/e94390953bc1/ijpr-09-379-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41c6/3870061/339884d83eed/ijpr-09-379-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41c6/3870061/289be1d4646d/ijpr-09-379-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41c6/3870061/7bfaec7ae4e7/ijpr-09-379-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41c6/3870061/e94390953bc1/ijpr-09-379-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41c6/3870061/339884d83eed/ijpr-09-379-g004.jpg

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