title: The synthesis and biological activity of a highly selective adenosine A2a receptor agonist.
abstract: Three novel nucleosides 1, 2, and 3 were prepared that contained side chains at the 2-position of adenosine. Compound 1 was shown to be the most selective A2a receptor agonist reported to date having an A1/A2 ratio of 2400. In addition, compound 1 was shown to reduce blood pressure in rats and dogs with only minimal effects on heart rate.
authors.affiliation: Hoechst Marion Roussel, Inc., Bridgewater, NJ 08807, USA.
authors.forename: D R
authors.initials: DR
authors.lastname: Borcherding
authors.forename: N L
authors.initials: NL
authors.lastname: Lentz
authors.forename: P M
authors.initials: PM
authors.lastname: Weintraub
authors.forename: M W
authors.initials: MW
authors.lastname: Dudley
authors.forename: R
authors.initials: R
authors.lastname: Secrest
authors.forename: P R
authors.initials: PR
authors.lastname: Kastner
authors.forename: N P
authors.initials: NP
authors.lastname: Peet
mesh_terms: D000241:Adenosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D004285:Dogs; D006339:Heart Rate / Q000187:drug effects; D006973:Hypertension / Q000503:physiopathology; D066298:In Vitro Techniques; D011684:Purine Nucleosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D058906:Purinergic P1 Receptor Agonists; D051381:Rats; D043705:Receptor, Adenosine A2A
chemical_list: C403763:2-((1-phenylpropyl)amino)adenosine; C403762:2-((phenylisopropyl)amino)adenosine; D011684:Purine Nucleosides; D058906:Purinergic P1 Receptor Agonists; D043705:Receptor, Adenosine A2A; D000241:Adenosine