Importance of making available selective adenosine receptor antagonists is boosted by recent findings of adenosine involvement in many CNS dysfunctions. In the present work a series of 8-bromo-9-alkyl adenines are prepared and fully characterized in radioligand binding assays or functional cyclase experiments in respect to their interaction with all the four adenosine receptor subtypes. Results show that the presence of the bromine atom in 8-position of 9-substituted adenines promotes in general the interaction with the adenosine receptors, in particular at the A_2A subtype. The present study also demonstrates that adenine derivatives could be a good starting point to obtain selective adenosine A_2B receptor antagonists.

腺苷参与许多中枢神经系统功能障碍的最新发现增强了提供选择性腺苷受体拮抗剂的重要性。在本工作中，制备了一系列8-溴-9-烷基腺嘌呤，并在放射性配体结合测定或功能环化酶实验中对其与所有四种腺苷受体亚型的相互作用进行了全面表征。结果表明，在9-取代的腺嘌呤的8位上的溴原子的存在通常促进与腺苷受体的相互作用，特别是在A _2A亚型处。本研究还表明，腺嘌呤衍生物可能是获得选择性腺苷A _2B受体拮抗剂的良好起点。