The dog saphenous vein: a sensitive and selective preparation for the Y2 receptor of neuropeptide Y.
The dog saphenous vein responds to neuropeptide Y with a dose-dependent contraction and this vasopressor effect is not altered by the removal of the endothelium nor by the neuropeptide Y Y1 receptor antagonist, BIBP 3226 ((R)-N2-(diphenylacetyl)-N-[(n-hydroxyphenyl)methyl]-argininami de). The dose-response curves obtained with neuropeptide Y, peptide YY and with C-terminal fragments such as neuropeptide Y-(2-26), neuropeptide Y-(13-36) and peptide YY-(3-36) have similar slopes and maxima. EC50 values of these compounds vary between 30 +/- 10 and 89 +/- 47 nM. The neuropeptide Y Y1 receptor-selective agonist [Leu31,Pro34]neuropeptide Y and human pancreatic polypeptide are inactive up to 1 microM. This pharmacological profile suggests that the contraction of the dog saphenous vein induced by neuropeptide Y and its homologues or fragments is mediated by a neuropeptide Y Y2 receptor type. Moreover, this neuropeptide Y Y2 receptor appears to be localized in the venous smooth muscle, where it exerts a direct myotropic effect that may be useful for the pharmacological characterization of new compounds acting as agonists or antagonists of the neuropeptide Y Y2 receptor.
Pheng
L H
LH
Department of Pharmacology, Medical School, Université de Sherbrooke, Québec, Canada.
Fournier
A
A
Dumont
Y
Y
Quirion
R
R
Regoli
D
D
D000818:Animals; D001120:Arginine / Q000031:analogs & derivatives / Q000494:pharmacology; D001681:Biological Assay; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D008297:Male; D009478:Neuropeptide Y / Q000494:pharmacology*; D010446:Peptide Fragments / Q000494:pharmacology; D019894:Peptide YY; D010455:Peptides / Q000037:antagonists & inhibitors / Q000494:pharmacology; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors / Q000378:metabolism*; D012501:Saphenous Vein / Q000187:drug effects*; D013045:Species Specificity; D013552:Swine; D014661:Vasoconstriction / Q000187:drug effects*
C092926:BIBP 3226; D009478:Neuropeptide Y; D010446:Peptide Fragments; D010455:Peptides; D017476:Receptors, Neuropeptide Y; D019894:Peptide YY; D001120:Arginine