[D-Trp(34)] neuropeptide Y is a potent and selective neuropeptide Y Y(5) receptor agonist with dramatic effects on food intake.
The neuropeptide Y (NPY) Y(5) receptor has been proposed to mediate several physiological effects of NPY, including the potent orexigenic activity of the peptide. However, the lack of selective NPY Y(5) receptor ligands limits the characterization of the physiological roles of this receptor. Screening of several analogs of NPY revealed that [D-Trp(34)]NPY is a potent and selective NPY Y(5) receptor agonist. Unlike the prototype selective NPY Y(5) receptor agonist [D-Trp(32)]NPY, [D-Trp(34)]NPY markedly increases food intake in rats, an effect that is blocked by the selective NPY Y(5) receptor antagonist CGP 71683A. These data demonstrate that [D-Trp(34)]NPY is a useful tool for studies aimed at determining the physiological roles of the NPY Y(5) receptor.
Parker
E M
EM
Department of CNS and Cardiovascular Research, Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. eric.parker@spcorp.com
Balasubramaniam
A
A
Guzzi
M
M
Mullins
D E
DE
Salisbury
B G
BG
Sheriff
S
S
Witten
M B
MB
Hwa
J J
JJ
D000818:Animals; D001667:Binding, Competitive; D016466:CHO Cells; D002460:Cell Line; D006224:Cricetinae; D000242:Cyclic AMP / Q000378:metabolism; D002149:Energy Intake / Q000187:drug effects*; D006801:Humans; D007700:Kinetics; D008297:Male; D009281:Naphthalenes / Q000494:pharmacology; D009478:Neuropeptide Y / Q000031:analogs & derivatives / Q000494:pharmacology*; D011743:Pyrimidines / Q000494:pharmacology; D051381:Rats; D020318:Rats, Long-Evans; D017476:Receptors, Neuropeptide Y / Q000819:agonists* / Q000378:metabolism; D011994:Recombinant Proteins / Q000819:agonists; D014162:Transfection
C412628:D-Trp(34) neuropeptide Y; D009281:Naphthalenes; D009478:Neuropeptide Y; D011743:Pyrimidines; D017476:Receptors, Neuropeptide Y; D011994:Recombinant Proteins; C100568:neuropeptide Y5 receptor; C116786:CGP 71683 A; D000242:Cyclic AMP