Labeling of A1 adenosine receptors in porcine atria with the antagonist radioligand 8-cyclopentyl-1,3-[3H]dipropylxanthine.
We have used the antagonist radioligand 8-cyclopentyl-1,3-[3H]dipropylxanthine to label adenosine recognition sites in porcine atrial membranes. 8-Cyclopentyl-1,3-[3H]dipropylxanthine bound saturably, reversibly and with high affinity to an apparently homogeneous population of recognition sites with a Bmax of 32.0 +/- 0.9 fmol/mg protein and a KD of 0.394 +/- 0.049 nM. Prototypic adenosine receptor agonists inhibited the specific binding of 8-cyclopentyl-1,3-[3H]dipropylxanthine in a manner consistent with the labeling of an A1 adenosine receptor. 8-Cyclopentyl-1,3-[3H]dipropylxanthine appears to be a valuable antagonist radioligand for the characterization of cardiac adenosine receptors.
Leid
M
M
College of Pharmacy, Oregon State University, Corvallis.
Franklin
P H
PH
Murray
T F
TF
D000818:Animals; D066298:In Vitro Techniques; D008024:Ligands; D009206:Myocardium / Q000378:metabolism*; D011869:Radioligand Assay; D011983:Receptors, Purinergic / Q000378:metabolism*; D013552:Swine; D014970:Xanthines
D008024:Ligands; D011983:Receptors, Purinergic; D014970:Xanthines; C051360:1,3-dipropyl-8-cyclopentylxanthine