Abstract
Characterization of 5-HT 4 receptors started in the late eighties following the important finding that the potent 5-HT3 receptor antagonist, tropisetron, could act as a competitive antagonist at the newly discovered 5-HT4 receptor. During recent years several pharmaceutical companies claimed that their 5-HT4 antagonists might be useful for the treatment and / or prophylaxis of cardiovascular, CNS and gastrointestinal disorders. This paper reviews the development of 5-HT4 receptor antagonists from experimental tools towards potential therapeutic agents.
Keywords: 5-ht4 receptor, 5-ht4 receptor antagonist, serotonin antagonist