Labeling of A1 adenosine receptors in porcine atria with the antagonist radioligand 8-cyclopentyl-1,3-[3H]dipropylxanthine

Mark Leid; Paul H. Franklin; Thomas F. Murray

doi:10.1016/0014-2999(88)90644-9

Labeling of A₁ adenosine receptors in porcine atria with the antagonist radioligand 8-cyclopentyl-1,3-[³H]dipropylxanthine

Mark Leid, Paul H. Franklin, Thomas F. Murray

Research output: Contribution to journal › Article › peer-review

16 Scopus citations

Abstract

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 homogenous population of recognition sites with a B_max of 32.0 ± 0.9 fmol/mg protein and a K_D of 0.394 ± 0.049 nM. Prototypic adenosine receptor agonists inhibited the specific binding of 8-cyclopentyl-1,3-[³H]dipropylxanthi 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.

Original language	English (US)
Pages (from-to)	141-144
Number of pages	4
Journal	European Journal of Pharmacology
Volume	147
Issue number	1
DOIs	https://doi.org/10.1016/0014-2999(88)90644-9
State	Published - Feb 16 1988
Externally published	Yes

All Science Journal Classification (ASJC) codes

Pharmacology

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10.1016/0014-2999(88)90644-9

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title = "Labeling of A1 adenosine receptors in porcine atria with the antagonist radioligand 8-cyclopentyl-1,3-[3H]dipropylxanthine",

abstract = "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 homogenous 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]dipropylxanthi 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.",

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AU - Murray, Thomas F.

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N2 - 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 homogenous 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]dipropylxanthi 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.

AB - 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 homogenous 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]dipropylxanthi 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.

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