2-SUBSTITUTED PI SYSTEM DERIVATIVES OF ADENOSINE THAT ARE CORONARY VASODILATORS ACTING VIA THE A_2A ADENOSINE RECEPTOR

Abstract

Compound 20 (CVT-3146 - a 2-[(N-1-(4-N-methylcarboxamidopyrazolyl)] adenosine derivative) and compound 31 (CVT-3033 - a 2-[(4-(1-N-pentyl-pyrazolyl)] adenosine derivative), were found to be short acting functionally selective coronary vasodilators (CV t_0.5 = 5.2 ± 0.2 and 3.4 ± 0.5 min, respectively - rat isolated heart 50% reversal time) with good potency (EC₅₀s = 6.4 ± 1.2 nM and 67.9 ± 16.7 nM, respectively), but they possess low affinity for the ADO A_2A receptor (K_i = 1122 ± 323 nM and 2138 ± 952 nM, respectively; pig striatum).

Acknowledgments