5-HT4 Receptors

Author(s): J Bockaert, S Claeysen, V Compan, A Dumuis

Journal Name: Current Drug Targets - CNS & Neurological Disorders
Continued as CNS & Neurological Disorders - Drug Targets

Volume 3 , Issue 1 , 2004


Serotonin 4 receptors (5-HT4Rs) were discovered 15 years ago. They are codedby a very complex gene (700Kb, 38 exons) which generates eight carboxy-terminalvariants (a, b, c, d, e, f, g, n). Their sequences differ after position L358. Another variant ischaracterized by a 14 residue insertion within the extracellular loop 2. Highly selectivepotent 5-HT4 receptor antagonists and partial agonists which cross the blood-brain barrier have been synthesized, but a specific full agonist for brain studiesis still missing. Based on physiological and behavioral experiments, 5-HT4Rs may be targets to treatcognitive 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 ordementia.

Keywords: 5-ht4 receptors, splice variants, g proteins, neurotransmitter release, cognition, pain, anxiety, feeding, cns drug targets

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Article Details

Year: 2004
Page: [39 - 51]
Pages: 13
DOI: 10.2174/1568007043482615

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