Section Review—Central & Peripheral Nervous Systems: The Evolution of Selective 5-HT_ID Receptor Antagonists

Abstract

Since their discovery in the late 1980s, 5-HT_1D receptors have aroused considerable interest, not least because they represent the most abundant 5-HT₁ receptor subtype in the CNS. Until recently, studies of the 5-HT_1D receptor have relied upon poorly selective agents and this has seriously hampered efforts to define their physiological and potential pathological role in the CNS. Now, a series of centrally active, selective 5-HT_1D receptor antagonists have become available which should add an important dimension to the study of 5-HT_1D receptors. This review provides background biology on 5-HT_1D receptors and the current status of novel chemical entities.