Chronic theophylline exposure increases agonist and antagonist binding to A1 adenosine receptors in rat brain

R. C. Sanders, Thomas F. Murray

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Abstract

Chronic treatment of rats with theophylline (75 mg/kg twice-daily for 21 consecutive days) significantly increased the specific binding of [3HCHA and [3H]DPCPX in cerebral cortical membranes. The absolute increase in the number of binding sites following theophylline treatment was approximately the same for each ligand, although this number represents a larger percentage of the total sites available to [3H]CHA. Saturation analysis of [3H]DPCPX binding indicated that theophylline treatment increased the maximum number of binding sites from 799 ± 13 to 920 ± 22 fmol/mg protein, while the affinity of [3H]DPCPX for A1 receptors was unaltered.These results suggest that chronic theophylline exposure produces both an increase in the number of A1 adenosine receptors and an enhancement of coupling of these receptors to G proteins.

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All Science Journal Classification (ASJC) codes

  • Cellular and Molecular Neuroscience
  • Drug Discovery
  • Pharmacology

Cite this

Chronic theophylline exposure increases agonist and antagonist binding to A1 adenosine receptors in rat brain. / Sanders, R. C.; Murray, Thomas F.

In: Neuropharmacology, Vol. 27, No. 7, 1988, p. 757-760.

Research output: Contribution to journalArticle