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

  title={Conjugation of a brain-penetrant peptide with neurotensin provides antinociceptive properties.},
  author={M. Demeule and N. Beaudet and A. R{\'e}gina and {\'E}. Besserer-Offroy and A. Murza and Pascal T{\'e}treault and K. Belleville and Christian Ch{\'e} and A. Larocque and Carine Thiot and R. B{\'e}liveau and J. Longpr{\'e} and {\'E}. Marsault and R. Leduc and J. Lachowicz and S. L. Gonias and J. Castaigne and P. Sarret},
  journal={The Journal of clinical investigation},
  volume={124 3},
  • M. Demeule, N. Beaudet, +15 authors P. Sarret
  • Published 2014
  • Medicine
  • The Journal of clinical investigation
  • Neurotensin (NT) has emerged as an important modulator of nociceptive transmission and exerts its biological effects through interactions with 2 distinct GPCRs, NTS1 and NTS2. NT provides strong analgesia when administered directly into the brain; however, the blood-brain barrier (BBB) is a major obstacle for effective delivery of potential analgesics to the brain. To overcome this challenge, we synthesized chemical conjugates that are transported across the BBB via receptor-mediated… CONTINUE READING
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