セロトニンレセプタ-
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概要
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The existence of two different functional receptors for 5-hydroxytryptamine (5-HT) was first proposed by Gaddum and Picarelli. Aided by the development of radioligand binding techniques, the heterogeneity of 5-HT receptors has become more apparent in the past ten years. There are three main types of 5-HT receptors: 5-HT<SUB>1</SUB>, 5-HT<SUB>2</SUB> and 5-HT<SUB>3</SUB>. Moreover, 5-HT, is heterogenous and can be divided into 5-HT<SUB>1A</SUB>, 5-HT<SUB>1B</SUB>, 5-HT<SUB>1C</SUB> and 5-HT<SUB>1D</SUB> subtypes. 5-HT<SUB>1B</SUB> is probably related to the 5-HT autoreceptor controlling 5-HT release. Multiple 5-HT receptors are differentially distributed throughout the brain, and the agonist-receptor interaction is altered by physical parameters and chemicals, suggesting that the receptors may be physiologically relevant. Three 5-HT receptor subtypes, 5-HT<SUB>1A</SUB>, 5-HTIC and 5-HT<SUB>2</SUB>, have been cloned. All three receptors contain approximately 450 amino acids arrayed as seven transmembrane domains. 5-HT<SUB>1</SUB> and 5-HT<SUB>1A</SUB> are coupled to adenylate cyclase positively and negatively, respectively, while 5-HTIC and 5-HT<SUB>2</SUB> are coupled positively to phospholipase C. 5-HT<SUB>1A</SUB> is also coupled to the opening of K<SUP>+</SUP> channels in hippocampal pyramidal cells. A number of 5-HT-induced physiological responses have been shown to correlate with the 5-HT receptor subtypes. Based on a number of pharmacological studies, it seems likely that the mode of action of certain psychotropic drugs is closely related to the activity of central 5-HT receptors.
- 社団法人 日本薬理学会の論文
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