Neuropeptide S is a 20-amino acid peptide that functions as an agonist through activation of its cognate GPCR receptor system. Modulation of the Neuropeptide S (NPS) receptor has been associated with a variety of disease states including anxiety, panic disorder, narcolepsy, PTSD, and importantly substance abuse.  Through comprehensive chemical modification and analog synthesis we have now defined a comprehensive NPS antagonist pharmacophore using traditional medicinal chemistry and computational/scaffold hopping approaches.  The compounds developed in our laboratory are highly potent at blocking NPS receptors in vitro using a calcium mobilization functional assay and are also active in rodent models of cocaine self-administration, stress induced, cue induced, and drug induced reinstatement.  Further modification and testing of these analogs will be of significant value in determining the comprehensive role of NPS in modulating substance abuse behaviors.

Development of novel tools to study the neuropeptide S system in models of substance abuse.

245th National Meeting (2013)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.