Characterization of biochemical effects of CGS 21680C, an A2-adenosine receptor agonist, in the mammalian ventricle

Journal of Cardiovascular Pharmacology
P BoknikH Wenzlaff

Abstract

Effects of a putative A2-adenosine receptor agonist 2-[(p-2-carboxyethyl)-phenethylamino]-5'-N-ethyl-carboxamide-adeno sine (CGS 21680C) on force of contraction, protein phosphorylation, cyclic adenosine monophosphate (cAMP) content, and the activity of phosphodiesterase (PDE) isoenzymes in guinea pig ventricular (GPV) preparations were studied. CGS 21680C (1-100 microM) did not affect force of contraction in isolated electrically driven papillary muscles and was ineffective in increasing phosphorylation of phospholamban (PLB) and the inhibitory subunit of troponin (TnI) in [32P]-labeled GPV cardiomyocytes. However, under the same conditions, CGS 21680C (10 microM) increased cAMP content from 4.3 +/- 0.2 to 13.0 +/- 0.6 pmol/mg protein, and this effect was completely abolished by A2-adenosine receptor antagonist 9-chloro-2-(2-furanyl)-5,6-dihydro-1,2,4-triazolo-(1,5-c)quinazolin++ +-5-imine (CGS 15943A). CGS 21680C (10 microM) inhibited PDE isoenzymes I, II, III, IV by 7.0, 8.3, 4.7, and 23.2%, respectively. Similarly, rolipram (100 microM), a selective PDE IV inhibitor, increased cAMP content from 4.4 +/- 0.3 to 7.2 +/- 0.3 pmol/mg protein without affecting the phosphorylation state of PLB and TnI. We conclude that CGS 21680C ...Continue Reading

References

Sep 1, 1992·British Journal of Pharmacology·T BethkeH Wenzlaff
Jan 3, 1991·European Journal of Pharmacology·A WilkenU Schwabe
Jan 1, 1991·Pharmacology & Therapeutics·W J Thompson
Dec 1, 1989·Naunyn-Schmiedeberg's Archives of Pharmacology·J NeumannB Stein
Sep 1, 1987·Naunyn-Schmiedeberg's Archives of Pharmacology·D MartensU Schwabe
Oct 1, 1988·Naunyn-Schmiedeberg's Archives of Pharmacology·B C MillarB J McDermott
Jul 16, 1986·Biochemical and Biophysical Research Communications·M B Anand-Srivastava, M Cantin
Jan 19, 1971·Biochemistry·W J Thompson, M M Appleman
May 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·C LondosJ Wolff
Mar 1, 1994·Journal of Molecular and Cellular Cardiology·B SteinC Seeland
Jul 1, 1993·The American Journal of Physiology·E F Bond, A M Gordon
Aug 1, 1993·Circulation·S Ballin, C Louis
Jun 1, 1993·Journal of Molecular and Cellular Cardiology·B SteinH Scholz

❮ Previous
Next ❯

Citations

Nov 13, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Ulrich GergsStephanie Läer
Nov 28, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Ulrich GergsJoachim Neumann
Dec 22, 1999·British Journal of Pharmacology·J NeumannW Schmitz
Feb 23, 2018·Naunyn-Schmiedeberg's Archives of Pharmacology·Juliano Q D RodriguesRosely O Godinho
Aug 2, 2003·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Marie GeorgetRodolphe Fischmeister
Mar 29, 2001·Physiological Reviews·G Vassort
Feb 9, 2002·American Journal of Physiology. Heart and Circulatory Physiology·Eric L KilpatrickRobert D Lasley
Mar 15, 2001·American Journal of Physiology. Heart and Circulatory Physiology·R D LasleyR M Mentzer
Feb 13, 2001·American Journal of Physiology. Heart and Circulatory Physiology·P BokníkJ Neumann
Oct 18, 2019·Frontiers in Pharmacology·Peter BoknikJoachim Neumann
Feb 13, 2021·Frontiers in Pharmacology·P BoknikU Gergs

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antihypertensive Agents: Mechanisms of Action

Antihypertensive drugs are used to treat hypertension (high blood pressure) which aims to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Discover the latest research on antihypertensive drugs and their mechanism of action here.