Discrimination between neuropeptide Y and peptide YY in the rat tail artery by the neuropeptide Y1-selective antagonist, BIBP 3226

British Journal of Pharmacology
H GicquiauxB Bucher

Abstract

1. The ability of the novel, nonpeptide, neuropeptide Y (NPY) Y1-selective antagonist, BIBP 3226 ¿(R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl)methyl]-D-arginine amide¿, to antagonize the increase in perfusion pressure induced by NPY and peptide Y (PYY) was tested in the perfused rat tail artery, a postjunctional Y1-receptor bioassay, precontracted by 1 microM phenylephrine. 2. NPY and PYY produced a concentration-dependent enhancement of the vasoconstrictor response evoked by 1 microM phenylephrine. Although NPY and PYY are roughly equipotent, the maximal contractile response elicited by PYY was about twice that elicited by NPY. 3. Increasing concentrations of BIBP 3226 caused a parallel and rightward shift in the NPY concentration-response curve without depressing the maximal response. The contractile effect of NPY was potently inhibited in a competitive manner. The pA2 value for BIBP 3226 was 7.01 +/- 0.08, a value equivalent to that observed in the rabbit saphenous vein. Although increasing concentrations of BIBP 3226 shifted the concentration-response curve of PYY to the right without any significant decrease in the maximal vasoconstrictor response, the antagonism appeared non-competitive as the slope of the Schild plot was...Continue Reading

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Citations

Jul 11, 2002·European Journal of Pharmacology·Rickard E Malmström
Apr 4, 1998·European Journal of Pharmacology·S P DucklesD N Krause
Jul 21, 1998·European Journal of Pharmacology·A Franco-Cereceda, J Liska
Mar 22, 2000·British Journal of Pharmacology·Y DumontR Quirion
Jan 13, 2001·British Journal of Pharmacology·H M CoxN D Holliday
Jul 3, 2009·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Gary J HodgesJ Kevin Shoemaker
Jan 3, 2009·PLoS Genetics·Svati H ShahElizabeth R Hauser
Jun 20, 2012·Future Medicinal Chemistry·Jessica V Mankus, Christopher R McCurdy
Nov 24, 2004·British Journal of Pharmacology·Dolores PrietoMedardo Hernández
Nov 26, 2010·Advances in Physiology Education·Christopher D Johnson
May 14, 2003·American Journal of Physiology. Heart and Circulatory Physiology·Eamonn BradleyChristopher D Johnson
Oct 22, 2003·Vascular Pharmacology·Tatsuru TsurumakiHiroshi Higuchi

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