[TRP11]-neurotensin and xenopsin discriminate between rat and guinea-pig neurotensin receptors

Life Sci. 1982 Sep 13;31(11):1145-50. doi: 10.1016/0024-3205(82)90089-3.

Abstract

The binding and biological activities of neurotensin and two analogues, [TRP11]-neurotensin and xenopsin, in which a tryptophan replaces the neurotensin residue Tyr11, were compared in rat and guinea-pig. The binding activity of three peptides was measured as their ability to inhibit the binding of [3H]neurotensin to rat and guinea-pig brain synaptic membranes. Their biological activities were measured as their effects on the contractility of rat and guinea-pig ileal smooth muscle preparations. In binding as well as biological assays, it was found that [Trp11]-neurotensin and xenopsin were as potent as neurotensin in the rat. In contrast, the two analogues were about 10 times less potent than neurotensin in the guinea-pig. These findings reveal differences between rat and guinea-pig neurotensin receptors should be considered when comparing the activity of neurotensin analogues in assays using tissue preparations from various animal species.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Binding, Competitive
  • Guinea Pigs
  • Muscle Contraction / drug effects
  • Muscle, Smooth / drug effects
  • Neurotensin / analogs & derivatives*
  • Neurotensin / analysis
  • Neurotensin / metabolism*
  • Oligopeptides / metabolism*
  • Peptides
  • Rats
  • Receptors, Neurotransmitter / metabolism*
  • Species Specificity
  • Xenopus Proteins*

Substances

  • Oligopeptides
  • Peptides
  • Receptors, Neurotransmitter
  • Xenopus Proteins
  • Neurotensin
  • xenopsin
  • neurotensin, Trp(11)-