Analogs of caffeine: antagonists with selectivity for A2 adenosine receptors.
Analogs of caffeine: antagonists with selectivity for A2 adenosine receptors.
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咖啡因类似物：对 A2 腺苷受体具有选择性的拮抗剂。
DOI：
10.1016/0024-3205(86)90023-8
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发表时间：
1986
期刊：
影响因子：
6.1
通讯作者：
John W. Daly
中科院分区：
文献类型：
--
作者：
Dieter Ukena;M. Shamim;W. Padgett;John W. Daly
咖啡因的几种类似物已被研究为A2腺苷受体的拮抗剂，其刺激大鼠嗜铬细胞瘤PC 12细胞和人血小板膜中的腺苷酸环化酶，以及A1腺苷受体的拮抗剂，其抑制大鼠脂肪细胞中的腺苷酸环化酶。在这些类似物中，1-炔丙基-3，7-二甲基黄嘌呤对PC 12细胞和血小板的A2受体的作用比咖啡因强约4- 7倍，7-丙基-1，3-二甲基黄嘌呤强约3- 4倍。在脂肪细胞的A1受体，这两种化合物的效力比咖啡因低约2倍。这些咖啡因类似物具有约10-20的A1/A2选择性比，并且是迄今报道的第一个选择性A2受体拮抗剂。为进一步开发高效、高选择性的腺苷A2受体拮抗剂奠定了基础。
Several analogs of caffeine have been investigated as antagonists at A2adenosine receptors stimulatory to adenylate cyclase in membranes from rat pheochromocytoma PC12 cells and human platelets and at A1adenosine receptors inhibitory to adenylate cyclase from rat fat cells. Among these analogs, 1-propargyl-3,7-dimethylxanthine was about 4- to 7-fold and 7-propyl-1,3-dimethylxanthine about 3- to 4-fold more potent than caffeine at A2receptors of PC12 cells and platelets. At A1receptors of fat cells, both compounds were about 2-fold less potent than caffeine. These caffeine analogs have an A1/A2selectivity ratio of about 10–20 and are the first selective A2receptor antagonists yet reported. The results may provide the basis for the further development of highly potent and highly selective A2adenosine receptor antagonists.
影响因子：
3.6
作者：
K. Jacobson;K. Kirk;W. Padgett;J. Daly
通讯作者：
K. Jacobson;K. Kirk;W. Padgett;J. Daly