A [ 3H]amine congener of 1,3-dipropyl-8-phenylxanthine : A new radioligand for A2 adenosine receptors of human platelets

Abstract

A xanthine amine congener (XAC), an amine-functionalized derivative of 1,3-dipropyl-8-phenylxanthine, is an antagonist ligand for A2 adenosine receptors of human platelets. XAC inhibited 5'- N-ethylcarboxamidoadenosine (NECA)-induced stimulation of adenylate cyclase activity with a K B of 24 nM. [ 3H]XAC exhibits saturable, specific binding with a K d of 12 nM and a B max of 1.1 pmol mg protein at 37°C. [ 3H]XAC binding in platelets is the first example of labeling of A2 adenosine receptors in which the potencies of adenosine agonists and antagonists in inhibiting binding are commensurate with their potencies at these receptors in functional studies. Furthermore, [ 3H]XAC is the first antagonist radioligand with high affinity at A2 adenosine receptors.