ZP120 causes relaxation by pre-junctional inhibition of noradrenergic neurotransmission in rat mesenteric resistance arteries

British Journal of Pharmacology
U SimonsenJørgen S Petersen

Abstract

ZP120 (Ac-RYYRWKKKKKKK-NH(2)), is a new partial nociceptin/orphanin FQ (NOP) receptor agonist with sodium-potassium sparing aquaretic effects. The mechanisms of vasodilatation of ZP120 were examined in rat mesenteric resistance arteries. Arterial segments (internal diameters 206+/-4 microm, n=224) were mounted in microvascular myographs for isometric tension recordings and electrical field stimulation (EFS). ZP120 and the endogenous NOP receptor ligand, N/OFQ, did not relax arteries contracted with noradrenaline or adenosine-triphosphate. EFS-evoked contractions were inhibited by a purinoceptor antagonist, suramin, and the alpha(1)-adrenoceptor antagonist prazosin. N/OFQ inhibited, concentration-dependently, EFS-evoked contractions with a maximal effect of 52+/-3% (n=8) at 1 microM. The maximal effect of 1 microM ZP120 was lower (27+/-5%, P<0.05, n=9) than for N/OFQ. Endothelial removal or pretreatment with capsaicin did not influence the vasodilator effects of ZP120 and N/OFQ. ZP120 and N/OFQ responses were preserved in the presence of suramin. The alpha(2)-adrenoceptor antagonist, rauwolscine, antagonized the effect of clonidine and brimonidine, but ZP120 and N/OFQ inhibition of EFS-evoked contraction was unaltered. The compe...Continue Reading

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Citations

May 29, 2013·Pharmacology & Therapeutics·Elaine Cristina Gavioli, Girolamo Calo'
Apr 24, 2010·British Journal of Anaesthesia·J McDonaldD G Lambert
Dec 9, 2010·British Journal of Anaesthesia·A Serrano-GomezD G Lambert
Nov 2, 2016·British Journal of Pharmacology·Inmaculada C VillarAdrian J Hobbs
Aug 2, 2008·Nature Reviews. Drug Discovery·David G Lambert
Feb 2, 2010·American Journal of Physiology. Lung Cellular and Molecular Physiology·Christel KroigaardUlf Simonsen
May 26, 2010·CNS Neuroscience & Therapeutics·Girolamo Calo'Remo Guerrini
Oct 2, 2009·Peptides·Richard J Bodnar

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