The synthesis and biological activity of a highly selective adenosine A2a receptor agonist.
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.
Borcherding
D R
DR
Hoechst Marion Roussel, Inc., Bridgewater, NJ 08807, USA.
Lentz
N L
NL
Weintraub
P M
PM
Dudley
M W
MW
Secrest
R
R
Kastner
P R
PR
Peet
N P
NP
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
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