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Characterization of cardiac A1 adenosine receptors by ligand binding and photoaffinity labeling.

Publication ,  Journal Article
Leung, E; Kwatra, MM; Hosey, MM; Green, RD
Published in: J Pharmacol Exp Ther
March 1988

[125I]N6-(p-aminobenzyl)adenosine and [125I]N6-(p-azidobenzyl)adenosine, which are potent agonists at A1 (Ri) adenosine receptors, have been used to characterize the adenosine receptor in membranes prepared from newborn chick heart. Scatchard analyses of [125I]N6-(p-aminobenzyl)adenosine binding to cardiac membranes revealed that the ligand bound to two affinity states of the receptor with Kd values of 0.7 and 9.9 nM. The corresponding maximum binding (Bmax) values were 25 and 86 fmol/mg of protein, respectively. In the presence of 0.1 mM 5'-guanylyl imidodiphosphate, a single affinity state was detected with a Kd of 9.4 nM and a Bmax of 96 fmol/mg of protein. Direct and indirect ligand binding studies with several adenosine receptor agonists and antagonists were used to compare the characteristics of the cardiac receptor with those of the A1 receptor in the cerebellum. The binding properties of the receptors in the two tissues were very similar although marked differences were observed in the binding kinetics of [125I]N6-(p-azidobenzyl)adenosine. Photo-affinity labeling experiments followed by sodium dodecyl sulfate-gel electrophoresis showed that the cardiac receptor had a apparent molecular weight of 37,600, which was slightly but significantly higher than that of the cerebellar receptor (35,500). The present results show that the cardiac receptor has ligand binding properties and a minimal subunit molecular weight similar to the more thoroughly studied A1 receptor in neural tissue.

Duke Scholars

Published In

J Pharmacol Exp Ther

ISSN

0022-3565

Publication Date

March 1988

Volume

244

Issue

3

Start / End Page

1150 / 1156

Location

United States

Related Subject Headings

  • Receptors, Purinergic
  • Radioligand Assay
  • Pharmacology & Pharmacy
  • Myocardium
  • Lithium
  • In Vitro Techniques
  • Guanylyl Imidodiphosphate
  • Chickens
  • Cerebellum
  • Azides
 

Citation

APA
Chicago
ICMJE
MLA
NLM
Leung, E., Kwatra, M. M., Hosey, M. M., & Green, R. D. (1988). Characterization of cardiac A1 adenosine receptors by ligand binding and photoaffinity labeling. J Pharmacol Exp Ther, 244(3), 1150–1156.
Leung, E., M. M. Kwatra, M. M. Hosey, and R. D. Green. “Characterization of cardiac A1 adenosine receptors by ligand binding and photoaffinity labeling.J Pharmacol Exp Ther 244, no. 3 (March 1988): 1150–56.
Leung E, Kwatra MM, Hosey MM, Green RD. Characterization of cardiac A1 adenosine receptors by ligand binding and photoaffinity labeling. J Pharmacol Exp Ther. 1988 Mar;244(3):1150–6.
Leung, E., et al. “Characterization of cardiac A1 adenosine receptors by ligand binding and photoaffinity labeling.J Pharmacol Exp Ther, vol. 244, no. 3, Mar. 1988, pp. 1150–56.
Leung E, Kwatra MM, Hosey MM, Green RD. Characterization of cardiac A1 adenosine receptors by ligand binding and photoaffinity labeling. J Pharmacol Exp Ther. 1988 Mar;244(3):1150–1156.

Published In

J Pharmacol Exp Ther

ISSN

0022-3565

Publication Date

March 1988

Volume

244

Issue

3

Start / End Page

1150 / 1156

Location

United States

Related Subject Headings

  • Receptors, Purinergic
  • Radioligand Assay
  • Pharmacology & Pharmacy
  • Myocardium
  • Lithium
  • In Vitro Techniques
  • Guanylyl Imidodiphosphate
  • Chickens
  • Cerebellum
  • Azides