PMID: 8938664Nov 1, 1996Paper

Opioid receptor agonists activate pertussis toxin-sensitive G proteins and inhibit adenylyl cyclase in canine cardiac sarcolemma

Naunyn-Schmiedeberg's Archives of Pharmacology
F NiroomandW Kübler

Abstract

Although both opioid receptors and endogenous opioids are abundant in cardiac tissues, the signal transduction pathways of opioids in cardiac sarcolemmal membranes have yet to be identified. In highly purified canine cardiac sarcolemmal membranes, binding of the opioid receptor antagonist [3H]diprenorphine and effects of mu, delta and kappa agonists on low Km GTPase and adenylyl cyclase were measured. Equilibrium binding of [3H]diprenorphine revealed a maximal binding capacity of 7.2 pmol/mg protein and a Kd of 1.3 nmol/l. In the presence of GTP, (D-Pen2,5, p-Cl-Phe4) enkephalin and (D-Arg6) dynorphin A 1-13 fragment both inhibited adenylyl cyclase by 20-25% (from 206 +/- 30 to 164 +/- 28 pmol.min-1.mg protein-1, EC50 6 mumol/L, and from 254 +/- 109 to 204 +/- 90 pmol.min-1.mg protein-1, EC50 8 mumol/L, respectively; P < 0.001). Both substances stimulated low Km GTPase by 20% and 13%, respectively (from 12.7 +/- 3.0 to 15.2 +/- 3.7 pmol.min-1.mg protein-1, EC50 12 mumol/L, P < 0.01, and from 9.1 +/- 2.8 to 10.4 +/- 3.2 pmol.min-1.mg protein-1, EC50 6 mumol/L, P < 0.05, respectively). These effects were blocked by the opioid receptor antagonist naltrexone and by pretreatment of sarcolemmal membranes with pertussis toxin. The mu ...Continue Reading

Citations

Jan 5, 2000·The Annals of Thoracic Surgery·C F SchwartzS F Bolling
Apr 24, 2001·Pharmacology & Therapeutics·J E Schultz, G J Gross
Jan 1, 1997·Peptides·G A OlsonA J Kastin
Dec 15, 2005·Heart, Lung & Circulation·Olivier W V van den BrinkSalvatore Pepe
Oct 25, 2003·Journal of Cardiovascular Pharmacology·Jason D KiltsMadan M Kwatra
Jun 18, 2002·The Journal of Biological Chemistry·Jason D KiltsMadan M Kwatra
Sep 5, 2019·Medical Sciences : Open Access Journal·Tyler C BeckThomas A Dix

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