The synthesis and biological activity of a highly selective adenosine A(2a) receptor agonist

Authors
Borcherding, DR Lentz, NL Weintraub, PM Dudley, MW Secrest, R Kastner, PR Peet, NP
Citation
Dr. Borcherding et al., The synthesis and biological activity of a highly selective adenosine A(2a) receptor agonist, NUCLEOS NUC, 18(10), 1999, pp. 2175-2191
Citations number
13
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES & NUCLEOTIDES
ISSN journal
07328311 → ACNP
Volume
18
Issue
10
Year of publication
1999
Pages
2175 - 2191
Database
ISI
SICI code
0732-8311(1999)18:10<2175:TSABAO>2.0.ZU;2-P
Abstract
Three novel nucleosides 1, 2, and 3 were prepared that contained side chain s at the 2-position of adenosine. Compound I was shown to be the most selec tive A(2a) receptor agonist reported to date having an A(1)/A(2) ratio of 2 400. In addition, compound 1 was shown to reduce blood pressure in rats and dogs with only minimal effects on heart rate.