Müller Christa E, Jacobson Kenneth A
University of Bonn, Pharmaceutical Institute, An der Immenburg 4, 53121, Bonn, Germany.
Handb Exp Pharmacol. 2011(200):151-99. doi: 10.1007/978-3-642-13443-2_6.
The natural plant alkaloids caffeine and theophylline were the first adenosine receptor (AR) antagonists described in the literature. They exhibit micromolar affinities and are non-selective. A large number of derivatives and analogues were subsequently synthesized and evaluated as AR antagonists. Very potent antagonists have thus been developed with selectivity for each of the four AR subtypes.
天然植物生物碱咖啡因和茶碱是文献中最早描述的腺苷受体（AR）拮抗剂。它们表现出微摩尔级的亲和力且无选择性。随后合成了大量衍生物和类似物，并作为AR拮抗剂进行评估。因此，已经开发出了对四种AR亚型中的每一种都具有选择性的强效拮抗剂。
