Characterization and assignment of uniformly labeled NT(8–13) at the agonist binding site of the G-protein coupled neurotensin receptor

Abstract

The neurotensin receptor is a member of the G-protein coupled receptor (GPCR) family of transmembrane proteins that is activated upon the binding of the basic tridecapeptide agonist, neurotensin, to the extracellular surfaces of cells. The neurotensin receptor is found widely in both the central nervous system and the periphery. In the periphery, it stimulates smooth muscle contraction [1,2]. In the central nervous system, it mediates a variety of activities including antinociception, hypothermia and increased locomoter activity [3–5]. These effects are probably mediated through the regulation of the mesolimbic and negrostriatal dopamine pathways [6,7]. As a result, the pharmacological action of the neurotensin is similar to that observed for dopamine, where compounds function as antipsychotics [6,7], and intervention may provide useful insights for the development of treatments for conditions such as schizophrenia [8] and Parkinson’s disease [9].