Peripherally Selective Cannabinoid 1 Receptor (CB1R) Agonists for the Treatment of Neuropathic Pain

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 w...

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Veröffentlicht in:	Journal of medicinal chemistry 2016-08, Vol.59 (16), p.7525-7543
Hauptverfasser:	Seltzman, Herbert H, Shiner, Craig, Hirt, Erin E, Gilliam, Anne F, Thomas, Brian F, Maitra, Rangan, Snyder, Rod, Black, Sherry L, Patel, Purvi R, Mulpuri, Yatendra, Spigelman, Igor
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals CHO Cells Cricetulus Dogs Dose-Response Relationship, Drug Humans Male Molecular Structure Neuralgia - drug therapy Rats Rats, Sprague-Dawley Receptor, Cannabinoid, CB1 - agonists Receptor, Cannabinoid, CB2 - agonists Structure-Activity Relationship
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Zusammenfassung:	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
ISSN:	0022-2623 1520-4804
DOI:	10.1021/acs.jmedchem.6b00516