The small peptide neurotensin is a potent regulator of dopamine signaling and can provide dramatic pain relief; however, the blood brain barrier provides a substantial challenge toward clinical use of neurotensin for analgesia.

In this issue of the Journal of Clinical Investigation, Philippe Sarret and colleagues at Université de Sherbrooke generated a conjugate of neurotensin with a peptide able to cross the blood brain barrier and evaluated the analgesic effects of this molecule in animal models of pain.

The authors observed efficient transportation of the conjugate (ANG2002) across the blood brain barrier and dose-dependent pain relief in multiple models. The results from this study suggest that ANG2002 has potential to be effective for clinical pain management.

TITLE: Conjugation of a brain-penetrant peptide with neurotensin provides antinociceptive properties