Ontology highlight
ABSTRACT:
SUBMITTER: Seltzman HH
PROVIDER: S-EPMC5474949 | biostudies-literature | 2016 Aug
REPOSITORIES: biostudies-literature
Seltzman Herbert H HH Shiner Craig C Hirt Erin E EE Gilliam Anne F AF Thomas Brian F BF Maitra Rangan R Snyder Rod R Black Sherry L SL Patel Purvi R PR Mulpuri Yatendra Y Spigelman Igor I
Journal of medicinal chemistry 20160810 16
Alleviation of neuropathic pain by cannabinoids is limited by their central nervous system (CNS) side effects. Indole and indene compounds were engineered for high hCB1R affinity, peripheral selectivity, metabolic stability, and in vivo efficacy. An epithelial cell line assay identified candidates with <1% blood-brain barrier penetration for testing in a rat neuropathy induced by unilateral sciatic nerve entrapment (SNE). The SNE-induced mechanical allodynia was reversibly suppressed, partially ...[more]