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在人类反复接触苯环己哌啶(PCP)后,大脑中的PCP和西格玛受体不会发生改变。

PCP and sigma receptors in brain are not altered after repeated exposure to PCP in humans.

作者信息

Weissman A D, Casanova M F, Kleinman J E, De Souza E B

机构信息

Neuroscience Branch, National Institute on Drug Abuse, Baltimore, MD 21224.

出版信息

Neuropsychopharmacology. 1991 Feb;4(2):95-102.

PMID:1851014
Abstract

The psychotomimetic effects of phencyclidine (PCP) in humans can persist or reappear months after the drug has been eliminated, suggesting that PCP can induce long-term changes in the brain. The present study examined whether repeated exposure to PCP in a human drug-addicted population was accompanied by alterations in either PCP or sigma binding sites in their postmortem brains as compared to suicide controls. Saturation studies using [3H]TCP and [3H]haloperidol in the presence of spiperone to measure PCP and sigma sites, respectively, revealed no significant differences in the affinity or density of binding sites between these two clinical populations in a variety of brain areas examined. The results suggest that these brain binding sites remain unperturbed in humans despite multiple challenges with PCP. Delayed psychotic episodes following the use of PCP may be attributed to other neurochemical changes that are initiated by interactions of PCP with these two binding sites.

摘要

苯环利定(PCP)对人类的拟精神病作用在药物消除数月后仍可能持续或再次出现,这表明PCP可诱导大脑发生长期变化。本研究调查了与自杀对照组相比,在人类吸毒成瘾人群中反复接触PCP是否伴随着其死后大脑中PCP或西格玛结合位点的改变。分别使用[3H]TCP和[3H]氟哌啶醇在螺哌隆存在的情况下进行饱和研究以测量PCP和西格玛位点,结果显示在检查的多个脑区中,这两个临床人群之间结合位点的亲和力或密度没有显著差异。结果表明,尽管多次接触PCP,但人类大脑中的这些结合位点并未受到干扰。使用PCP后出现的延迟性精神病发作可能归因于PCP与这两个结合位点相互作用引发的其他神经化学变化。

相似文献

1
PCP and sigma receptors in brain are not altered after repeated exposure to PCP in humans.在人类反复接触苯环己哌啶(PCP)后,大脑中的PCP和西格玛受体不会发生改变。
Neuropsychopharmacology. 1991 Feb;4(2):95-102.
2
Differential regulation of sigma and PCP receptors after chronic administration of haloperidol and phencyclidine in mice.小鼠长期给予氟哌啶醇和苯环己哌啶后σ受体和PCP受体的差异调节
FASEB J. 1989 May;3(7):1868-72. doi: 10.1096/fasebj.3.7.2541039.
3
Phencyclidine and sigma receptors in rat spinal cord: binding characterization and quantitative autoradiography.大鼠脊髓中的苯环己哌啶与西格玛受体:结合特性及定量放射自显影
Synapse. 1989;4(1):1-10. doi: 10.1002/syn.890040102.
4
In vivo binding of [3H]d-N-allylnormetazocine and [3H]haloperidol to sigma receptors in the mouse brain.
J Chem Neuroanat. 1990 Sep-Oct;3(5):347-54.
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Characterization and autoradiographic visualization of (+)-[3H]SKF10,047 binding in rat and mouse brain: further evidence for phencyclidine/"sigma opiate" receptor commonality.大鼠和小鼠脑中(+)-[³H]SKF10,047结合的表征及放射自显影可视化:苯环己哌啶/“σ阿片样物质”受体共性的进一步证据
J Pharmacol Exp Ther. 1986 May;237(2):681-8.
6
Interaction of L-glutamate and magnesium with phencyclidine recognition sites in rat brain: evidence for multiple affinity states of the phencyclidine/N-methyl-D-aspartate receptor complex.L-谷氨酸和镁与大鼠脑内苯环利定识别位点的相互作用:苯环利定/N-甲基-D-天冬氨酸受体复合物多种亲和状态的证据。
Mol Pharmacol. 1987 Dec;32(6):820-30.
7
Pharmacological specificity of some psychotomimetic and antipsychotic agents for the sigma and PCP binding sites.
Life Sci. 1988;42(7):745-52. doi: 10.1016/0024-3205(88)90646-7.
8
Pharmacological and autoradiographic discrimination of sigma and phencyclidine receptor binding sites in brain with (+)-[3H]SKF 10,047, (+)-[3H]-3-[3-hydroxyphenyl]-N-(1-propyl)piperidine and [3H]-1-[1-(2-thienyl)cyclohexyl]piperidine.用(+)-[³H]SKF 10,047、(+)-[³H]-3-[3-羟基苯基]-N-(1-丙基)哌啶和[³H]-1-[1-(2-噻吩基)环己基]哌啶对脑中σ和苯环利定受体结合位点进行药理学和放射自显影鉴别。
J Pharmacol Exp Ther. 1986 Aug;238(2):739-48.
9
Biochemical and behavioral effects of sigma and PCP ligands.σ受体配体和苯环己哌啶类似物的生化及行为效应
Synapse. 1988;2(3):240-3. doi: 10.1002/syn.890020311.
10
Initial identification and characterization of sigma receptors on human peripheral blood leukocytes.人外周血白细胞上σ受体的初步鉴定与表征
J Pharmacol Exp Ther. 1988 Dec;247(3):1114-9.

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