Prolonged exposure to 5'-N-ethylcarboxamidoadenosine (NECA) does not affect the adenosine A2A-mediated vasodilation in porcine coronary arteries

Pharmacological Research : the Official Journal of the Italian Pharmacological Society
A ContiA Monopoli

Abstract

At present, four distinct adenosine receptors (A1, A2A, A2B, and A3) have been cloned and characterized in several species. It is known that prolonged exposure of tissues to receptor agonists induces A1 receptor desensitization. However, controversial data are reported on whether or not prolonged stimulation of A2A adenosine receptors induces tolerance. Using the porcine coronary artery, a sensitive vascular model, studies were designed, with the aim to clarify how prolonged exposure to the adenosine agonist 5'-N-ethylcarboxamidoadenosine (NECA) affects A2A receptor responsiveness. The arteries were precontracted with PGF2alpha (3 microM) and cumulative dose-response curves to either NECA itself, or the selective A2A agonists, 2-[4-2(2-carboxyethyl)phenethylamino]-5'-N-ethylcarboxamidoadenosi ne (CGS 21680) and 2-hexynyl-5'-N-ethylcarboxamidoadenosine (2HE-NECA) were obtained. In separate experiments, coronary rings were incubated with NECA (10 microM) for 30 min or 2 h. After 2 h washout period, functional response was assessed. The arteries showed high sensitivity to adenosine agonist-induced vasorelaxation. EC50 (nM) values were 71.8 (35.5-145), 20.0 (11.2-32.7) and 40.2 (20.4-79.1) for NECA, 2HE-NECA and CGS 21680, respecti...Continue Reading

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Citations

Oct 7, 2010·Inflammation Research : Official Journal of the European Histamine Research Society ... [et Al.]·Xiao-pei Gao, Israel Rubinstein
Mar 28, 2008·Purinergic Signalling·Elisabeth C KlaasseMargot W Beukers
Jun 18, 1999·British Journal of Pharmacology·B K Kemp, T M Cocks
Sep 28, 2007·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Gabriela E GarciaLili Feng
Nov 26, 2003·Journal of Cardiovascular Pharmacology·Moez Rekik, Jamal S Mustafa
Oct 16, 2018·Cardiovascular & Hematological Disorders Drug Targets·Trevor SimardBenjamin Hibbert
Feb 13, 2021·Frontiers in Pharmacology·P BoknikU Gergs

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