Abstract
5-HT4 receptors have a unique pharmacology. In addition to indole derivatives, two agonist classes have been discovered, benzamides and benzimidazolones. Classical 5-HT receptor antagonists are generally inactive on this receptor. Three antagonists have been described and derive from each class of agonist (ICS 205 930, SDZ 205 557, DAU 6285). 5-HT4 receptors increase cAMP formation and, depending on the cell, inhibit K+ channels (neurons) or activate Ca2+ channels (human cardiomyocytes).
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