5-Hydroxytryptamine Receptor Subtypes and their Modulators with Therapeutic Potentials

Abstract

5-hydroxytryptamine (5-HT) has become one of the most investigated and complex biogenic amines. The main receptors and their subtypes, e.g., 5-HT_I (5-HT_1A, 5-HT_1B, 5-HT_ID, 5-HT_IE and 5-HT_1F), 5-HT₂ (5-HT_2A, 5-HT_2B and 5-HT_2C), 5-HT₃, 5-HT₄, 5-HT₅ (5-HT_5A, 5-HT_5B), 5-HT₆ and 5-HT₇ have been identified. Specific drugs which are capable of either selectively stimulating or inhibiting these receptor subtypes are being designed. This has generated therapeutic potentials of 5-HT receptor modulators in a variety of disease conditions. Conditions where 5-HT receptor modulators have established their use with distinct efficacy and advantages include migraine, anxiety, psychosis, obesity and cancer therapy-induced vomiting by cytotoxic drugs and radiation. Discovery of 5-HT, its biosynthesis, metabolism, physiological role and the potential of 5-HT receptor modulators in various nervous, cardiovascular and gastrointestinal tract disorders, bone growth and micturition have been discussed in this article.

doi:10.4021/jocmr2009.05.1237

Publish ahead of print May 18, 2009