Receptor binding at two different temperatures to discriminate agonist and antagonist behaviour of adenosine A1 receptor ligands in rat brain

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Abstract
The inhibitory binding constants, Ki, at the adenosine A1 receptor in rat brain have been measured at 0 and 25°C for 25 typical ligands. The Ki ratios at the two temperatures are greater and smaller than unity for adenosine agonists and xanthine antagonists, respectively. These results suggest that two-temperature measurements of in-vitro Ki constants represent a simple method of discriminating between in-vivo agonistic and antagonistic behaviour of A1 adenosine receptor ligands.