JMV 449: a pseudopeptide analogue of neurotensin-(8-13) with highly potent and long-lasting hypothermic and analgesic effects in the mouse.

Abstract

We recently reported that H-Lys psi (CH2NH)Lys-Pro-Tyr-Ile-Leu-OH (JMV 449), a pseudopeptide analogue of neurotensin-(8-13) with a reduced CH2NH bond in position 8-9, was about 3 times more potent than neurotensin in binding to mouse brain membranes and in contracting the guinea-pig ileum, and was markedly more resistant to degradation than neurotensin when exposed to rat brain membranes. In the present study, we compared the time courses and dose-response relationships for the ability of i.c.v. injected neurotensin and JMV 449 to elicit hypothermia and analgesia (tail-flick test) in the mouse. The results show that the pseudopeptide analogue behaved as a highly potent and long-lasting neurotensin agonist in these two in vivo bioassays. The analogue should prove very useful for studying the effects of chronic neurotensin receptor stimulation in vitro and in vivo.

• Authors: I Dubuc, J Costentin, S Doulut, M Rodriguez, J Martinez, P Kitabgi
• Journal: European journal of pharmacology (Eur J Pharmacol) Vol. 219 Issue 2 Pg. 327-9 (Aug 25 1992) ISSN: 0014-2999 [Print] Netherlands
• PMID: 1425958 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Analgesics
• Oligopeptides
• JMV 449
• Neurotensin

Topics

• Amino Acid Sequence
• Analgesics (pharmacology)
• Animals
• Guinea Pigs
• Hypothermia (chemically induced)
• Male
• Mice
• Molecular Sequence Data
• Neurotensin (pharmacology)
• Oligopeptides (administration & dosage, pharmacology)