This article reviews the medicinal implications of 5-HT4R in the peripheral and central nervous systems, based on data from two hundred bibliographic references. An exhaustive compilation of molecules reported to be antagonists or agonists for 5-HT4R is presented, including chemical structures, binding properties and pharmacological profiles. In the last part of the review, some key concepts concerning structure-activity relationships are highlighted.
Keywords: Serotonin, 5-HT4 receptor ligands, Agonists, Antagonists, Clinical applications
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