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. 2001 Apr-Jul;20(4-7):343-60.
doi: 10.1081/NCN-100002306.

2-substituted pi system derivatives of adenosine that are coronary vasodilators acting via the A2A adenosine receptor

J Zablocki  1 , V Palle, B Blackburn, E Elzein, G Nudelman, S Gothe, Z Gao, Z Li, S Meyer, L Belardinelli
Affiliations

2-substituted pi system derivatives of adenosine that are coronary vasodilators acting via the A2A adenosine receptor

J Zablocki et al. Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul.

Abstract

Compound 20 (CVT-3146--a 2-[(N-1-(4-N-methylcarboxamidopyrazolyl)] adenosine derivative) and compound 31 (CVT-3033--a 2-[(4-(1-N-pentylpyrazolyl)] adenosine derivative), were found to be short acting functionally selective coronary vasodilators (CV t0.5 = 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 A2A receptor (Ki = 1122 +/- 323 nM and 2138 +/- 952 nM, respectively; pig striatum).

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