Details

Autor(en) / Beteiligte

• PALLE, Venkata P
• VARKHEDKAR, Vaibhav
• KWAN LEUNG
• CHU, Nancy
• ZABLOCKI, Jeff A
• IBRAHIM, Prabha
• AHMED, Hiba
• ZHIHE LI
• ZHENHAI GAO
• OZECK, Mark
• YUZHI WU
• DEWAN ZENG
• LIN WU

Titel

Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor: efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2004-01, Vol.14 (2), p.535-539

Ort / Verlag

Oxford: Elsevier

Erscheinungsjahr

2004

Quelle

MEDLINE

Beschreibungen/Notizen

• The SAR for the affinity to the A(1) adenosine receptor and relative intrinsic efficacy (IE, [(35)S]-GTPgammaS 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 A(1) AdoR mediated effect. Progress towards obtaining a partial A(1) AdoR agonist to potentially control ventricular rate during atrial fibrillation has been made with the discovery of several potent partial A(1) AdoR agonists (compounds 13, 14, and 17).