MRS 5698 是一种选择性 Gi 蛋白偶联 A3 腺苷受体 (A3AR) 激动剂，对人和小鼠 A3AR 的 Kis 值分别约为 3 nM。
High affinity and selective A3 adenosine receptor agonist (Ki ~ 3 nM); displays >1000-fold selectivity over A1 and A2A adenosine receptors. Reverses mechanoallodynia in several neuropathic pain models in vivo. Orally bioavailable.
Little et al (2015) Endogenous adenosine A3 receptor activation selectively alleviates persistent pain states. Brain 138 28 PMID:25414036 |Tosh et al (2012) Structure-guided design of A3 adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions. J.Med.Chem. 55 4847 PMID:22559880 |Tosh et al (2015) Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain. Purinergic Signal. 11 371 PMID:26111639
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