Effects of some organophosphorus compounds on the binding of a radioligand (8-cyclopentyl 1, 3-[3H]dipropylxanthine) to adenosine receptors in ovine cardiac membranes.
8-Cyclopentyl-1,3-[3H] dipropylxanthine [( 3H]CPX) is a potent radioligand that specifically binds to the A1 adenosine receptors. Its high specificity makes it a suitable ligand for the characterization of A1 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 A1 adenosine receptors in ovine cardiac membranes with Ki values of 36.7, 328 and 175 microM, 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 A1 adenosine receptors.
Lau
W M
WM
Materials Research Laboratory, Department of Defence, Ascot Vale, Victoria, Australia.
Szilagyi
M
M
Freeman
S E
SE
D000818:Animals; D002800:Cholinesterase Inhibitors / Q000633:toxicity*; D066298:In Vitro Techniques; D009206:Myocardium / Q000378:metabolism*; D010755:Organophosphates / Q000633:toxicity*; D015221:Potassium Channels / Q000187:drug effects; D011983:Receptors, Purinergic / Q000187:drug effects / Q000378:metabolism*; D012524:Sarin / Q000633:toxicity*; D012756:Sheep; D012999:Soman / Q000633:toxicity*; D014970:Xanthines / Q000378:metabolism*
D002800:Cholinesterase Inhibitors; D010755:Organophosphates; D015221:Potassium Channels; D011983:Receptors, Purinergic; D014970:Xanthines; D012999:Soman; C051360:1,3-dipropyl-8-cyclopentylxanthine; D012524:Sarin; C009374:tabun