Serotonin agonists and antagonists. Pharmacological tools and therapeutics

✍ Scribed by I. van Wijngaarden; M. Th. M. Tulp; W. Soudijn

• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 458 KB
• Volume: 112
• Category: Article
• ISSN: 0165-0513
• DOI: 10.1002/recl.19931120209

✦ Synopsis

Abstract

Medicinal chemists have provided crucial tools for the identification and characterization of various subtypes of serotonin (5‐hydroxytryptamine, 5‐HT) receptors. At present, potent and selective (ratio ≥ 100) ligands have been developed for the 5‐HT~1A~, 5‐HT~1B~ and 5‐HT~3~ receptor subtype. For the 5‐HT~1C~, 5‐HT~1D~, 5‐HT~1E~, 5‐HT~2~ and 5‐HT~4~ receptor subtypes, only potent, non‐selective compounds are available. In this paper, we present the affinities (obtained by radioligand binding studies) of the most selective tools known today for each of the 5‐HT subtypes and we describe some structure‐affinity relationships of a number of interesting compounds. The potential use of several of these selective ligands as pharmacological tools and therapeutics will be briefly reviewed.