Stimulation by neurotensin of (3H)5-hydroxytryptamine (5HT) release from rat frontal cortex slices

Neuropeptides. 1998 Oct;32(5):465-71. doi: 10.1016/s0143-4179(98)90073-7.

Abstract

The effect of neurotensin (NT) on the K+-evoked (3H)5HT release from brain frontal cortex slices was studied in rats. NT(1-13) and NT(8-13) increased (3H)5HT release with EC50 values in the nanomolar range and Emax values in the range of 100% of control, whereas D-tyr11-NT was inactive. Concerning NT receptor antagonists, SR 48692 and SR 142948A antagonized with IC50 values of 4.8+/-1.8 nM and 4.5+/-1.8 nM respectively, the NT stimulated K+-evoked (3H)5HT release. SR 48527 also antagonized NT induced (3H)5HT release with an IC50 value of 0.95+/-0.06 nM whereas the inactive R(-) enantiomer SR 49711 only inhibited this effect with IC50 value close to 10(-6)M. The 5HT-releasing effect of NT was completely inhibited by tetrodotoxin suggesting that NT receptors involved in the control of 5-HT release are not located on 5-HT terminals. After a first NT (10(-7)M) application, the NT (10(-7)M, 10(-6)M) effect under K+ depolarization was drastically decreased, indicating that the NT receptor could be desensitized. No potentiating effect of NT on K+-evoked (3H)5HT release was observed in striatal and hippocampal slices. These results suggest that, in the rat frontal cortex, NT regulates 5HT release through a high affinity NT receptor not associated with 5HT terminals.

MeSH terms

  • Adamantane / analogs & derivatives
  • Adamantane / pharmacology
  • Animals
  • Corpus Striatum / drug effects
  • Corpus Striatum / metabolism
  • Dizocilpine Maleate / pharmacology
  • Dopamine Antagonists / pharmacology
  • Down-Regulation
  • Frontal Lobe / drug effects
  • Frontal Lobe / metabolism*
  • Hippocampus / drug effects
  • Hippocampus / metabolism
  • Imidazoles / pharmacology
  • In Vitro Techniques
  • Inhibitory Concentration 50
  • Neurotensin / analogs & derivatives
  • Neurotensin / pharmacology*
  • Peptide Fragments / pharmacology
  • Potassium / pharmacology
  • Pyrazoles / pharmacology
  • Quinolines / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors
  • Receptors, Neurotensin / agonists
  • Receptors, Neurotensin / antagonists & inhibitors
  • Receptors, Neurotensin / physiology
  • Serotonin / metabolism*
  • Tetrodotoxin / pharmacology

Substances

  • Dopamine Antagonists
  • Imidazoles
  • Peptide Fragments
  • Pyrazoles
  • Quinolines
  • Receptors, N-Methyl-D-Aspartate
  • Receptors, Neurotensin
  • SR 142948A
  • SR 48527
  • SR 48692
  • Serotonin
  • Neurotensin
  • Tetrodotoxin
  • Dizocilpine Maleate
  • Adamantane
  • Potassium