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A [ 3 H]amine congener of 1,3‐dipropyl‐8‐phenylxanthine
Author(s) -
Ukena Dieter,
Jacobson Kenneth A.,
Kirk Kenneth L.,
Daly John W.
Publication year - 1986
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(86)80493-8
Subject(s) - chemistry , amine gas treating , receptor , adenosine , adenosine receptor , ligand (biochemistry) , stereochemistry , xanthine , platelet , antagonist , biochemistry , enzyme , agonist , biology , organic chemistry , immunology
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. [ 3 H]XAC exhibits saturable, specific binding with a K d of 12 nM and a B max of 1.1 protein at 37°C. [ 3 H]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, [ 3 H]XAC is the first antagonist radioligand with high affinity at A2 adenosine receptors.