Ontology highlight
ABSTRACT:
SUBMITTER: Tosh DK
PROVIDER: S-EPMC4266358 | biostudies-literature | 2014 Dec
REPOSITORIES: biostudies-literature
Tosh Dilip K DK Finley Amanda A Paoletta Silvia S Moss Steven M SM Gao Zhan-Guo ZG Gizewski Elizabeth T ET Auchampach John A JA Salvemini Daniela D Jacobson Kenneth A KA
Journal of medicinal chemistry 20141125 23
(N)-Methanocarba adenosine 5'-methyluronamides containing 2-arylethynyl groups were synthesized as A3 adenosine receptor (AR) agonists and screened in vivo (po) for reduction of neuropathic pain. A small N(6)-methyl group maintained binding affinity, with human > mouse A3AR and MW < 500 and other favorable physicochemical properties. Emax (maximal efficacy in a mouse chronic constriction injury pain model) of previously characterized A3AR agonist, 2-(3,4-difluorophenylethynyl)-N(6)-(3-chlorobenz ...[more]