R Volpini, E Camaioni, S Costanzi, S Vittori, K N Klotz, G Cristalli
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引用次数: 9
摘要
基于2-(己-1-炔基)腺苷-5'- n -乙脲酰胺(HENECA, 2)对大鼠腺苷受体具有良好的亲和力和不同程度的选择性，在N6-和/或5'位置取代的2-(己-1-炔基)腺苷衍生物进行了合成。所有新化合物都与最近克隆的人A1、A2A、A2B和A3腺苷受体进行了放射性配体结合和腺苷酸环化酶检测。
Synthesis of di- and tri-substituted adenosine derivatives and their affinities at human adenosine receptor subtypes.
The synthesis of 2-(hex-1-ynyl)adenosine derivatives substituted at the N6- and/or 5'-position was carried out on the basis that 2-(hex-1-ynyl)adenosine-5'-N-ethyluronamide (HENECA, 2) showed good affinity and different degree of selectivity for rat adenosine receptors. All new compounds were tested in radioligand binding and adenylyl cyclase assays with recently cloned human A1, A2A, A2B, and A3 adenosine receptors.
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