5-HT4 Receptors

被引：151

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

[1]

ANDRADE R, 1991, J PHARMACOL EXP THER, V257, P930

[2]

[Anonymous], 5 HT4 RECEPTORS BRAI, DOI DOI 10.1038/nrgastro.2012.32

[3]

ANSANAY H, 1992, MOL PHARMACOL, V42, P808

[4] CAMP-DEPENDENT, LONG-LASTING INHIBITION OF A K+ CURRENT IN MAMMALIAN NEURONS [J].

ANSANAY, H ;

DUMUIS, A ;

SEBBEN, M ;

BOCKAERT, J ;

FAGNI, L .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1995, 92 (14) :6635-6639

[5] 5-HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle [J].

Bach, T ;

Syversveen, T ;

Kvingedal, AM ;

Krobert, KA ;

Brattelid, T ;

Kaumann, AJ ;

Levy, FO .

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 2001, 363 (02) :146-160

[6] A review of central 5-HT receptors and their function [J].

Barnes, NM ;

Sharp, T .

NEUROPHARMACOLOGY, 1999, 38 (08) :1083-1152

[7] BENZIMIDAZOLONE DERIVATIVES ACT AS 5-HT4 RECEPTOR LIGANDS IN RAT ESOPHAGUS [J].

BAXTER, GS ;

CLARKE, DE .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1992, 212 (2-3) :225-229

[8] QUATERNIZED RENZAPRIDE AS A POTENT AND SELECTIVE 5-HT4 RECEPTOR AGONIST [J].

BAXTER, GS ;

BOYLAND, P ;

GASTER, LM ;

KING, FD .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (04) :633-634

[9] Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant [J].

Bender, E ;

Pindon, A ;

van Oers, I ;

Zhang, YB ;

Gommeren, W ;

Verhasselt, P ;

Jurzak, M ;

Leysen, J ;

Luyten, W .

JOURNAL OF NEUROCHEMISTRY, 2000, 74 (02) :478-489

[10] Dual effects of 5-HT4 receptor activation on GABA release from guinea pig hippocampal slices [J].

Bianchi, C ;

Rodi, D ;

Marino, S ;

Beani, L ;

Siniscalchi, A .

NEUROREPORT, 2002, 13 (17) :2177-2180

← 1 2 3 4 5 6 7 8 9 10 →