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Structure–activity relationships (SAR) of fused 1,2,4-triazolo[1,5-c ]pyrimidine were performed. Various substituents were introduced into the heterocyclic ring to improve the potency of adenosine A3 receptor binding affinity and A3-selectivity against other subtypes. Potent and selective A3 receptor antagonists were identified and were evaluated in a monkey model of intraocular pressure by eye-drop...
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