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(2) 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.
Malmström
Rickard E
RE
Division of Pharmacology, Department of Physiology and Pharmacology, Karolinska Institute, S-17177, Stockholm, Sweden. rickard.malmstrom@fyfa.ki.se
D000818:Animals; D002317:Cardiovascular Agents / Q000494:pharmacology*; D006801:Humans; D009478:Neuropeptide Y / Q000502:physiology; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*; D013564:Sympathetic Nervous System / Q000502:physiology; D009435:Synaptic Transmission / Q000502:physiology; D014661:Vasoconstriction / Q000502:physiology
D002317:Cardiovascular Agents; D009478:Neuropeptide Y; D017476:Receptors, Neuropeptide Y