2003•Central Nervous System Agents in Medicinal ChemistryRequires access

Serotonin Type-4 (5-HT4) Receptors as Therapeutic Targets: 5-HT4 Receptor Antagonists

Henri Mattes, Hans‐Juergen Pfannkuche

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

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Key concepts: 5-HT4 receptor, Tropisetron, Receptor antagonist, Antagonist, Receptor, Serotonin, Competitive antagonist, 5-HT receptor