Effects of some organophosphorus compounds on the binding of a radioligand (8-cyclopentyl 1, 3-[3H]dipropylxanthine) to adenosine receptors in ovine cardiac membranes
✍ Scribed by Wai-Man Lau; Maria Szilagyi; Shirley E. Freeman
- Publisher
- John Wiley and Sons
- Year
- 1991
- Tongue
- English
- Weight
- 417 KB
- Volume
- 11
- Category
- Article
- ISSN
- 0260-437X
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✦ Synopsis
8-Cy~lopentyl-l,3-[~H] dipropylxanthine (['HICPX
) is a potent radioligand that specifically binds to the A l adenosine receptors. Its high specificity makes it a suitable ligand for the characterization of A l adenosine receptors in tissues with low receptor densities. We have demonstrated that the organophosphorus compounds soman, tabun and sarin, at relatively high concentrations, all bind to the Al adenosine receptors in ovine cardiac membranes with Ki values of 36.7, 328 and 175 pM, respectively. The binding of soman to the receptor site was found to be totally reversible. We suggested that these organophosphorus compounds affect the mechanical responses of the heart through interaction with a potassium channel that does not seem to be closely linked to the A l adenosine receptors.