Pharmacology of neuropeptide Y receptor antagonists -: Focus on cardiovascular functions

Neuropeptide Y is one of the most abundant mammalian neuropeptides identified to date. The possible actions of neuropeptide Y, that is co-localized and released with noradrenaline, as a sympathetic co-transmitter has attracted much attention during the last decade. In recent years, several non-peptide antagonists with high subtype selectivity for neuropeptide Y receptors have been introduced. With them, the status of neuropeptide Y as a sympathetic transmitter has been established, and so have profound cardiovascular effects mediated by neuropeptide Y Y-1 and Y, receptors. Significant release of neuropeptide Y occurs especially upon stronger sympathetic activation, and recent data suggest that the importance of neuropeptide Y seems enhanced in stress-related cardiovascular disorders. The true significance of neuropeptide Y has thus started to unfold, owing to the presence of the first generation of selective neuropeptide Y receptor antagonists. This review concerns the pharmacology of these agents, what we have learnt from them, and might find out in the future. (C) 2002 Elsevier Science B.V. All rights reserved.