Ontology highlight
ABSTRACT:
SUBMITTER: Tosh DK
PROVIDER: S-EPMC4499829 | biostudies-other | 2015 Jul
REPOSITORIES: biostudies-other
Tosh Dilip K DK Crane Steven S Chen Zhoumou Z Paoletta Silvia S Gao Zhan-Guo ZG Gizewski Elizabeth E Auchampach John A JA Salvemini Daniela D Jacobson Kenneth A KA
ACS medicinal chemistry letters 20150520 7
Substitution of rigidified A3 adenosine receptor (AR) agonists with a 2-((5-chlorothiophen-2-yl)ethynyl) or a 2-(4-(5-chlorothiophen-2-yl)-1H-1,2,3-triazol-1-yl) group provides prolonged protection in a model of chronic neuropathic pain. These agonists contain a bicyclo[3.1.0]hexane ((N)-methanocarba) ring system in place of ribose, which adopts a receptor-preferred conformation. N (6)-Small alkyl derivatives were newly optimized for A3AR affinity and the effects of a 1-deaza-adenine modificatio ...[more]