title: 2-substituted pi system derivatives of adenosine that are coronary vasodilators acting via the A2A 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-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).
authors.affiliation: Tripos, Inc., San Francisco, California, USA.
authors.forename: J
authors.initials: J
authors.lastname: Zablocki
authors.forename: V
authors.initials: V
authors.lastname: Palle
authors.forename: B
authors.initials: B
authors.lastname: Blackburn
authors.forename: E
authors.initials: E
authors.lastname: Elzein
authors.forename: G
authors.initials: G
authors.lastname: Nudelman
authors.forename: S
authors.initials: S
authors.lastname: Gothe
authors.forename: Z
authors.initials: Z
authors.lastname: Gao
authors.forename: Z
authors.initials: Z
authors.lastname: Li
authors.forename: S
authors.initials: S
authors.lastname: Meyer
authors.forename: L
authors.initials: L
authors.lastname: Belardinelli
mesh_terms: D000241:Adenosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D001921:Brain / Q000378:metabolism; D003331:Coronary Vessels / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D008958:Models, Molecular; D058906:Purinergic P1 Receptor Agonists; D051381:Rats; D043705:Receptor, Adenosine A2A; D018047:Receptors, Purinergic P1 / Q000378:metabolism; D013329:Structure-Activity Relationship; D013552:Swine; D014665:Vasodilator Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D058906:Purinergic P1 Receptor Agonists; D043705:Receptor, Adenosine A2A; D018047:Receptors, Purinergic P1; D014665:Vasodilator Agents; D000241:Adenosine