吡唑并[3,4-d]嘧啶，一类新型腺苷拮抗剂。

Pyrazolo [3,4-d] pyrimidines, a new class of adenosine antagonists.

作者信息

Davies L P, Brown D J, Chow S C, Johnston G A

出版信息

Neurosci Lett. 1983 Oct 31;41(1-2):189-93. doi: 10.1016/0304-3940(83)90245-8.

Abstract

A variety of nitrogen heterocycles structurally related to caffeine and theophylline have been tested for activity as adenosine receptor antagonists. Preliminary screening, utilizing displacement of [3H]N6-phenylisopropyladenosine binding to rat brain membrane A1-adenosine receptors, identified several pyrazolo[3,4-d]pyrimidines with potential antagonist activity. These were then tested for their ability to antagonize the adenosine-stimulated adenylate cyclase system of guinea-pig brain slices. One of these, 4,6-bis-alpha-carbamoylethylthio-1-phenylpyrazolo[3,4-d]pyrimidine (DJB-KK), was over an order of magnitude more potent than theophylline in blocking adenosine-stimulated increases in cyclic AMP levels.

摘要

已对多种在结构上与咖啡因和茶碱相关的氮杂环化合物进行了测试，以评估其作为腺苷受体拮抗剂的活性。利用[³H]N⁶-苯基异丙基腺苷与大鼠脑膜A1-腺苷受体结合的置换进行初步筛选，确定了几种具有潜在拮抗剂活性的吡唑并[3,4-d]嘧啶。然后测试了它们拮抗豚鼠脑片腺苷刺激的腺苷酸环化酶系统的能力。其中一种化合物，4,6-双-α-氨甲酰基乙基硫基-1-苯基吡唑并[3,4-d]嘧啶（DJB-KK），在阻断腺苷刺激的环磷酸腺苷水平升高方面比茶碱强一个数量级以上。