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Neuropeptide S (NPS) is a 20-residue peptide and endogenous ligand of the NPS receptor (NPSR). This receptor was a formerly orphan GPCR whose activation increases calcium and cyclic adenosine monophosphate levels. The NPS/NPSR system is expressed in several brain regions where it controls important biological functions including locomotor activity, arousal and sleep, anxiety, food intake, memory, pain, and drug addiction.
The medicinal chemistry and pharmacology of both peptide and non-peptide modulators of the NPSR as a potential drug discovery target have been attentive investigating. Several potent NPSR antagonists are available as valuable pharmacological tools despite showing suboptimal pharmacokinetic properties in vivo. The optimization of these ligands is needed to speed up their potential clinical advancement as pharmaceuticals to treat drug addiction. Small-molecule NPSR agonists will allow investigation of the beneficial effects of selective NPSR activation in a large panel of psychiatric disorders and to foresee their therapeutic potential as anxiolytics, nootropics, and analgesics.
All chemotypes presented in the reference library have been investigated for common motives. The fragments, crucial for high potency have been predicted on the basement of literature review and expert opinion. (Among these moieties are hydrophobic or aromatic fragments and HBA).
