Müller C E, Grahner B, Heber D
Pharmazeutisches Institut, Universität Tübingen.
Pharmazie. 1994 Dec;49(12):878-80.
Two novel classes of adenosine receptor (AR) antagonists, 4-amino-1,8-naphthyridines and 5-aminopyrido[2,3-d]pyrimidines, have been identified and investigated in radioligand binding assays. The compounds exhibit affinities for A1 and A2a AR of rat brain in the micromolar range. 1,8-Naphthyridines are non-selective, or somewhat selective for either A1- or A2 AR. Pyrido[2,3-d]pyrimidines are several-fold selective for A1 AR, the most potent and selective compound being 5-n-butylamino-1,3-dimethyl-1,2,3,4-tetrahydropyrido-[2,3-d]pyr imi dine-2,4-dione (12) with a Ki value of 1.8 microM at A1 AR and greater than 10-fold A1-selectivity.
已鉴定出两类新型腺苷受体（AR）拮抗剂，即4-氨基-1,8-萘啶和5-氨基吡啶并[2,3-d]嘧啶，并通过放射性配体结合试验对其进行了研究。这些化合物对大鼠脑A1和A2a AR的亲和力在微摩尔范围内。1,8-萘啶对A1和A2 AR是非选择性的，或对其中一种有一定选择性。吡啶并[2,3-d]嘧啶对A1 AR有几倍的选择性，最有效和选择性最强的化合物是5-正丁基氨基-1,3-二甲基-1,2,3,4-四氢吡啶并[2,3-d]嘧啶-2,4-二酮（12），其在A1 AR处的Ki值为1.8 μM，且具有大于10倍的A1选择性。
