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The c-terminal neurotensin-(8-13) fragment potently modulates rat neostriatal dopamine-d(2) receptors

Academic Article
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Overview

authors

  • Li, X. M.
  • Voneuler, G.
  • Hedlund, Peter
  • Finnman, U. B.
  • Fuxe, K.

publication date

  • March 1993

journal

  • European Journal of Pharmacology  Journal

abstract

  • The effects of neurotensin fragments and of neurotensin itself on the characteristics of neostriatal dopamine D2 agonist binding were studied in competition experiments with dopamine using the D2 antagonist, [3H]raclopride. The biologically active neurotensin-(8-13) fragment, but not the inactive neurotensin-(1-7) fragment, caused a concentration-related increase in the KH and KL values of dopamine with a maximal increase by 110 and 97%, respectively, at 1 nM, while neurotensin-(1-13) only induced such changes at 10 nM. In view of the higher potency and the increased ability of neurotensin-(8-13) versus neurotensin (1-13) to reduce the affinities of the high- and low-affinity states of the neostriatal D2 receptors, the C-terminal neurotensin fragments may be among the endogenous ligands of the neostriatal neurotensin receptors.

subject areas

  • Animals
  • Binding, Competitive
  • In Vitro Techniques
  • Male
  • Neostriatum
  • Neurotensin
  • Peptide Fragments
  • Raclopride
  • Radioligand Assay
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine D2
  • Salicylamides
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Research

keywords

  • (RAT)
  • DOPAMINE-D(2) RECEPTORS
  • NEOSTRIATUM
  • NEUROTENSIN FRAGMENTS
  • RECEPTOR-RECEPTOR INTERACTIONS
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Identity

International Standard Serial Number (ISSN)

  • 0014-2999

Digital Object Identifier (DOI)

  • 10.1016/0014-2999(93)90716-u

PubMed ID

  • 8472756
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Additional Document Info

start page

  • 125

end page

  • 128

volume

  • 234

issue

  • 1

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