Affinity and intrinsic efficacy (IE) of 5′-carbamoyl adenosine analogues for the A 1 adenosine receptor—efforts towards the discovery of a chronic ventricular rate …

…, V Varkhedkar, P Ibrahim, H Ahmed, Z Li, Z Gao…

文献索引：Palle, Venkata P.; Varkhedkar, Vaibhav; Ibrahim, Prabha; Ahmed, Hiba; Li, Zhihe; Gao, Zhenhai; Ozeck, Mark; Wu, Yuzhi; Zeng, Dewan; Wu, Lin; Leung, Kwan; Chu, Nancy; Zablocki, Jeff A. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 2 p. 535 - 539

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被引用次数: 8

摘要

The SAR for the affinity to the A1 adenosine receptor and relative intrinsic efficacy (IE,[35S]- GTPγS binding) of a series of 5′-carbamate and 5′-thionocarbamate derivatives of tecadenoson is described. Based on this SAR, selected compounds were evaluated in guinea pig isolated hearts to determine whether they were partial or full agonists with respect to their negative dromotropism, an A1 AdoR mediated effect. Progress towards ...