5-HT4 Receptors

被引：148

作者：

Bockaert, J. ^{[1
]}

Claeysen, S. ^{[1
]}

Compan, V ^{[1
]}

Dumuis, A. ^{[1
]}

机构：

[1] CCIPE, UPR CNRS 2580, 141 Rue Cardonille, F-34094 Montpellier 5, France

来源：

CNS & NEUROLOGICAL DISORDERS-DRUG TARGETS | 2004年 / 3卷 / 01期

关键词：

5-HT4; receptors; Splice variants; G proteins; Neurotransmitter release; Cognition; Pain; Anxiety; Feeding; CNS drug targets;

D O I：

10.2174/1568007043482615

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

Serotonin 4 receptors (5-HT(4)Rs) were discovered 15 years ago. They are coded by a very complex gene (700Kb, 38 exons) which generates eight carboxy-terminal variants (a, b, c, d, e, f, g, n). Their sequences differ after position L-358. Another variant is characterized by a 14 residue insertion within the extracellular loop 2. Highly selective potent 5-HT4 receptor antagonists and partial agonists which cross the blood-brain barrier have been synthesized, but a specific full agonist for brain studies is still missing. Based on physiological and behavioral experiments, 5-HT(4)Rs may be targets to treat cognitive deficits, abdominal pain and feeding disorders. One 5-HT4R-directed drug (SL65.0155) is already in phase II to treat patients suffering from memory deficits or dementia.

引用

页码：39 / 51

页数：13

共 135 条

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