Binding of 2',5'-dideoxyadenosine to brain membranes. Comparison to P-site inhibition of adenylate cyclase

Biochemical Pharmacology
Y NimitJ W Daly

Abstract

Membranes from rat cerebral cortex and striatum contain a relatively large number of high-affinity binding sites for [3H]2',5'-dideoxyadenosine, [3H]adenine arabinoside, and [3H]adenosine. The binding of [3H]2',5'-dideoxyadenosine and [3H]adenine arabinoside was virtually unaffected by relatively specific agonists and antagonists for adenosine receptors, such as 2-chloroadenosine, N6-phenylisopropyladenosine or theophylline. Binding of [3H]adenosine was partially blocked by such receptor ligands. The specific binding of all three ligands was antagonized by a variety of adenosine analogs which inhibit adenylate cyclase by interaction with the so-called P-site associated with this enzyme. However, potencies of adenosine analogs as P-site inhibitors of adenylate cyclase and as antagonists of binding do not correlate well. 5'-Methylthioadenosine had high potency and efficacy versus binding of [3H]2',5'-dideoxyadenosine but had virtually no effect on activity of adenylate cyclase. 2-Fluoroadenosine was less potent than adenosine as an antagonist of specific binding of [3H]2',5'-dideoxyadenosine, while 2-fluoroderivatives of adenosine, adenine arabinoside and adenine xylofuranoside were more potent than the parent compounds as P-site...Continue Reading

References

Dec 1, 1979·Naunyn-Schmiedeberg's Archives of Pharmacology·U SchwabeT Trost
Dec 1, 1977·Proceedings of the National Academy of Sciences of the United States of America·C Londos, J Wolff
Nov 1, 1978·Archives of Biochemistry and Biophysics·J WolffG H Cook
Apr 1, 1974·Analytical Biochemistry·Y SalomonM Rodbell
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Sep 1, 1980·Naunyn-Schmiedeberg's Archives of Pharmacology·U Schwabe, T Trost
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May 1, 1980·Canadian Journal of Physiology and Pharmacology·P H WuB Rinaldi

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Citations

Oct 1, 1997·Drug Development Research·John W DalyKenneth A Jacobson
Feb 1, 1984·Naunyn-Schmiedeberg's Archives of Pharmacology·K SchmidtH P Baer
Jan 1, 1983·Progress in Neuro-psychopharmacology & Biological Psychiatry·M Williams
Oct 16, 2002·Anais Da Academia Brasileira De Ciências·Roberto Paes-De-Carvalho

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