Open Access5-HT4 Receptors
Author(s) -
J. Bockaert,
Sylvie Claeysen,
Valérie Compan,
Aline Dumuis
Publication year - 2004
Publication title -
current drug targets - cns and neurological disorders
Language(s) - English
Resource type - Journals
eISSN - 2212-5299
pISSN - 1568-007X
DOI - 10.2174/1568007043482615
Subject(s) - agonist , receptor , serotonin , partial agonist , exon , dementia , neuroscience , medicine , gene , chemistry , biology , biochemistry , disease
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-HT(4) 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-HT(4)R-directed drug (SL65.0155) is already in phase II to treat patients suffering from memory deficits or dementia.
Accelerating Research
Robert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom
Address
John Eccles HouseRobert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom