A [3H]amine congener of 1,3‐dipropyl‐8‐phenylxanthine

FEBS Letters

Jacobson, Kenneth A.¹  Kirk, Kenneth L.¹  Ukena, Dieter²  Daly, John W.² 

[1] Laboratory of Chemistry, National Institute of Arthritis, Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20205, USA;Laboratory of Bioorganic Chemistry National Institute of Arthritis, Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20205, USA

关键词: Adenosine receptor;    Platelet;    Xanthine;   

DOI  :  10.1016/0014-5793(86)80493-8

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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 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.

【 授权许可】

Unknown