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  • Title: 2-substituted pi system derivatives of adenosine that are coronary vasodilators acting via the A2A adenosine receptor.
    Author: Zablocki J, Palle V, Blackburn B, Elzein E, Nudelman G, Gothe S, Gao Z, Li Z, Meyer S, Belardinelli L.
    Journal: Nucleosides Nucleotides Nucleic Acids; 2001; 20(4-7):343-60. PubMed ID: 11563047.
    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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