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苯环利定、麦角酸二乙胺和三甲氧苯乙胺:脑动脉痉挛与致幻活性。

Phencyclidine, lysergic acid diethylamide, and mescaline: cerebral artery spasms and hallucinogenic activity.

作者信息

Altura B T, Altura B M

出版信息

Science. 1981 May 29;212(4498):1051-2. doi: 10.1126/science.7195070.

DOI:10.1126/science.7195070
PMID:7195070
Abstract

Phencyclidine (PCP), lysergic acid diethylamide (LSD), and mescaline produced potent contractile responses on isolated basilar and middle cerebral arteries, where, in terms of potency, LSD greater than mescaline greater than PCP. All three drugs produced cerebrovasospasm in a concentration range which parallels that needed for their psychotomimetic and intoxicating actions. Specific receptors for PCP, which subserve contraction and differ from those for LSD and mescaline, are found in cerebral arteries. Concentrations of PCP that produced near-maximum contractile responses on cerebral arteries were similar to those in the blood and brain of human subjects who had died from PCP overdoses. A specific calcium antagonist, verapamil, readily prevented (and reversed) PCP-induced vasospasm. This study provides direct evidence for PCP receptors in cerebral blood vessels, the biologic action of which can be reversed by a calcium antagonist; the clinical use of the latter could prove invaluable in treating PCP-intoxicated victims.

摘要

苯环利定(PCP)、麦角酸二乙酰胺(LSD)和三甲氧苯乙胺对离体的基底动脉和大脑中动脉产生强烈的收缩反应,就效力而言,LSD大于三甲氧苯乙胺大于PCP。这三种药物在一定浓度范围内都会引起脑血管痉挛,该浓度范围与其致幻和中毒作用所需的浓度范围相当。在脑动脉中发现了PCP的特异性受体,这些受体介导收缩作用,且与LSD和三甲氧苯乙胺的受体不同。在脑动脉上产生接近最大收缩反应的PCP浓度与死于PCP过量的人类受试者血液和大脑中的浓度相似。一种特异性钙拮抗剂维拉帕米能轻易预防(并逆转)PCP诱导的血管痉挛。这项研究为脑血管中的PCP受体提供了直接证据,其生物学作用可被钙拮抗剂逆转;后者在治疗PCP中毒受害者方面的临床应用可能被证明具有极高价值。

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Science. 1981 May 29;212(4498):1051-2. doi: 10.1126/science.7195070.
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Identification of benzomorphan-kappa opiate receptors in cerebral arteries which subserve relaxation.对负责舒张作用的脑动脉中苯并吗啡烷-κ阿片受体的鉴定。
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苯环利定(“天使粉”)类似物和西格玛阿片类苯并吗啡烷会导致脑动脉痉挛。
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