NOVEL DISCRIMINATORY LIGANDS FOR 5-HT2B RECEPTORS

The 5-HT2B receptor is the most recent addition to the 5-HT2 receptor family and shares strong operational similarities with the structurall y related 5-HT2A and 5-HT2C receptor subty;pes. The strength of the ph armacological association, particularly between 5-HT2B and 5-HT2C rece ptors, suggests a need to consider carefully the use of ligands which may now be regarded as somewhat non-selective for the receptors in thi s class. The possibility that biological activity previously supposed to involve 5-HT2C receptors may actually involve 5-HT2B receptors high lights a need to develop ligands with improved selectivity profiles. I n this regard, medicinal chemistry continues to provide novel ligands which, if truly selective, should facilitate our understanding of the physiology, pathophysiology and therapeutic potential of 5-HT2B recept or modulation. This article reviews some of the newest ligands which m ay be used in the discrimination and characterisation of 5 HT2B recept or function.