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磷酸肌醇系统相关的5-羟色胺受体亚型及其药理学特性与临床关联

Phosphoinositide system-linked serotonin receptor subtypes and their pharmacological properties and clinical correlates.

作者信息

Pandey S C, Davis J M, Pandey G N

机构信息

Department of Psychiatry, College of Medicine, University of Illinois at Chicago 60612, USA.

出版信息

J Psychiatry Neurosci. 1995 May;20(3):215-25.

PMID:7786883
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1188687/
Abstract

Serotonergic neurotransmission represents a complex mechanism involving pre- and post-synaptic events and distinct 5-HT receptor subtypes. Serotonin (5-HT) receptors have been classified into several categories, and they are termed as 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6 and 5-HT7 type receptors. 5-HT1 receptors have been further subdivided into 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E and 5-HT1F. 5-HT2 receptors have been divided into 5-HT2A, 5-HT2B and 5-HT2C receptors. All 5-HT2 receptor subtypes are linked to the multifunctional phosphoinositide (PI) signalling system. 5-HT3 receptors are considered ion-gated receptors and are also linked to the PI signalling system by an unknown mechanism. The 5-HT2A receptor subtype is the most widely studied of the 5-HT receptors in psychiatric disorders (for example, suicide, depression and schizophrenia) as well as in relation to the mechanism of action of antidepressant drugs. The roles of 5-HT2C and 5-HT3 receptors in psychiatric disorders are less clear. These 5-HT receptors also play an important role in alcoholism. It has been shown that 5-HT2A, 5-HT2C and 5-HT3 antagonists cause attenuation of alcohol intake in animals and humans. However, the exact mechanisms are unknown. The recent cloning of the cDNAs for 5-HT2A, 5-HT2C and 5-HT3 receptors provides the opportunity to explore the molecular mechanisms responsible for the alterations in these receptors during illness as well as pharmacotherapy. This review article will focus on the current research into the pharmacological properties, molecular biology, and clinical correlates of 5-HT2A, 5-HT2C and 5-HT3 receptors.

摘要

血清素能神经传递是一种复杂的机制,涉及突触前和突触后事件以及不同的5-羟色胺(5-HT)受体亚型。5-羟色胺(5-HT)受体已被分为几类,分别称为5-HT1、5-HT2、5-HT3、5-HT4、5-HT5、5-HT6和5-HT7型受体。5-HT1受体进一步细分为5-HT1A、5-HT1B、5-HT1D、5-HT1E和5-HT1F。5-HT2受体分为5-HT2A、5-HT2B和5-HT2C受体。所有5-HT2受体亚型都与多功能磷酸肌醇(PI)信号系统相连。5-HT3受体被认为是离子门控受体,并且也通过未知机制与PI信号系统相连。5-HT2A受体亚型是在精神疾病(例如自杀、抑郁症和精神分裂症)以及与抗抑郁药物作用机制相关方面研究最广泛的5-HT受体。5-HT2C和5-HT3受体在精神疾病中的作用尚不清楚。这些5-HT受体在酒精中毒中也起重要作用。已经表明,5-HT2A、5-HT2C和5-HT3拮抗剂可导致动物和人类酒精摄入量减少。然而,确切机制尚不清楚。最近5-HT2A、5-HT2C和5-HT3受体的cDNA克隆为探索疾病期间以及药物治疗过程中这些受体改变的分子机制提供了机会。这篇综述文章将聚焦于目前对5-HT2A、5-HT2C和5-HT3受体的药理特性、分子生物学及临床相关性的研究。

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Serotonin uptake sites and serotonin receptors are altered in the limbic system of schizophrenics.血清素摄取位点和血清素受体在精神分裂症患者的边缘系统中发生改变。
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Eur J Pharmacol. 1993 Sep 15;247(1):81-8. doi: 10.1016/0922-4106(93)90140-5.
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