Structure-antinociceptive activity of neurotensin and some novel analogues in the periaqueductal gray region of the brainstem

Nayef R.F. Al-Rodhan, Elliott Richelson, Judith A. Gilbert, Daniel J. McCormick, Kiyoko S. Kanba, Michael A. Pfenning, Al Nelson, Eric W. Larson, Tony L. Yaksh

Research output: Contribution to journalArticlepeer-review

81 Scopus citations

Abstract

Neurotensin, an endogenous tridecapeptide, produces a potent, naloxone-insensitive antinociceptive response when it is microinjected into the periaqueductal gray region of the rat brainstem. In the present study, the ED50 for neurotensin in inducing antinociception was 1.5 nmol, two times more potent than morphine. We sought to find whether neurotensin's antinociceptive effects were mediated by the same receptor that mediates its other functions. We found that the structure-activity relationship of neurotensin-induced antinociception was different from that required for the stimulation of intracellular cyclic GMP production in neuroblastoma clone N1E-115 and the binding to N1E-115 cells, human brain tissue, or rat periaqueductal gray. These data suggest there exists a subtype of neurotensin receptors in neural tissue that mediates its antinociceptive actions.

Original languageEnglish (US)
Pages (from-to)227-235
Number of pages9
JournalBrain Research
Volume557
Issue number1-2
DOIs
StatePublished - Aug 23 1991

Keywords

  • Antinociception
  • Neurotensin
  • Neurotensin receptor
  • Pain
  • Periaqueductal gray
  • Structure-activity relationship

ASJC Scopus subject areas

  • General Neuroscience
  • Molecular Biology
  • Clinical Neurology
  • Developmental Biology

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