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Article Dans Une Revue Neuropharmacology Année : 2008

5-HT4 receptors: History, molecular pharmacology and brain functions

Résumé

Twenty years ago, we started the characterization of a 5-HT receptor coupled to cAMP production in neurons. This receptor obviously had a different pharmacology to the other 5-HT receptors described at that time, i.e. the 5-HT1, 5-HT2, 5-HT3 receptors. We proposed to name it the 5-HT4 receptor. Nowadays, 5-HT4 receptors are one of the most studied GPCRs belonging to the "rhodopsin" family. Thanks to the existence of a great variety of ligands with inverse agonist, partial agonist, agonist and antagonist profiles , the pharmacological and physiological properties of this receptor are beginning to emerge. Although some 5-HT4 partial agonists have been on the market for gastro-intestinal pathologies, 5-HT4 receptor drugs have still to be commercialized for brain disorders. However, since 5-HT4 receptors have recognized effects on memory, depression and feeding in animal models, there is still hope for a therapeutic destiny of this interesting target in brain disorders.

Domaines

Neurobiologie
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Dates et versions

hal-01667629 , version 1 (20-02-2020)

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Joël Bockaert, Sylvie Claeysen, Valerie Compan, Aline Dumuis. 5-HT4 receptors: History, molecular pharmacology and brain functions. Neuropharmacology, 2008, 55 (6), pp.922-931. ⟨10.1016/j.neuropharm.2008.05.013⟩. ⟨hal-01667629⟩
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