Journal
CNS & NEUROLOGICAL DISORDERS-DRUG TARGETS
Volume 3, Issue 1, Pages 39-51Publisher
BENTHAM SCIENCE PUBL
DOI: 10.2174/1568007043482615
Keywords
5-HT4 receptors; Splice variants; G proteins; Neurotransmitter release; Cognition; Pain; Anxiety; Feeding; CNS drug targets
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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.
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