Simultaneous integration of both β<sup>3</sup>hLys<sup>8</sup> and 6-OH-Tic<sup>11</sup> into NT(8-13) produced a potent and NTS2-selective analogue with strong analgesic action after intrathecal delivery in the rat formalin-induced pain model with an ED<sub>50</sub> of 1.4 nmol.
Our results suggest that abnormalities in the opioid and neurotensin systems may underlie the increase in pain threshold found in suicide attempters, and possibly risk for suicidal behavior.
Neurotensin receptor 1 (NTSR1) is a G-protein-coupled receptor (GPCR) that engages multiple subtypes of G protein, and is involved in the regulation of blood pressure, body temperature, weight and the response to pain.
Under normal physiological conditions, neurotensin is involved in the regulation of pain, body temperature, physical activity, appetite as well as learning and memory.