Neurobiology of Disease A Novel Brain Penetrant NPS Receptor Antagonist, NCGC00185684, Blocks Alcohol-Induced ERK- Phosphorylation in the Central Amygdala and Decreases Operant Alcohol Self-Administration in Rats
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چکیده
Annika Thorsell,1,3* Jenica D. Tapocik,1* Ke Liu,2* Michelle Zook,1 Lauren Bell,1 Meghan Flanigan,1 Samarjit Patnaik,2 Juan Marugan,2 Ruslan Damadzic,1 Seameen J. Dehdashti,2 Melanie L. Schwandt,1 Noel Southall,2 Christopher P. Austin,2 Robert Eskay,1 Roberto Ciccocioppo,4 Wei Zheng,2* and Markus Heilig1 1Laboratory of Clinical and Translational Studies, National Institute on Alcohol Abuse and Alcoholism, Bethesda, Maryland 20892, 2National Center for Advancing Translational Sciences, Bethesda, Maryland 20892-3370, 3Department of Clinical and Experimental Medicine, Linköping University, 581 83 Linköping, Sweden, and 4School of Pharmacy, Pharmacology Unit, Camerino University, 62032 Camerino, Italy
منابع مشابه
A novel brain penetrant NPS receptor antagonist, NCGC00185684, blocks alcohol-induced ERK-phosphorylation in the central amygdala and decreases operant alcohol self-administration in rats.
The Neuropeptide S receptor, a Gs/Gq-coupled GPCR expressed in brain regions involved in mediating drug reward, has recently emerged as a candidate therapeutic target in addictive disorders. Here, we describe the in vitro and in vivo pharmacology of a novel, selective and brain penetrant NPSR antagonist with nanomolar affinity for the NPSR, NCGC00185684. In vitro, NCGC00185684 shows biased anta...
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تاریخ انتشار 2013