Literature DB >> 8075852

The nonpeptide neurotensin antagonist, SR 48692, used as a tool to reveal putative neurotensin receptor subtypes.

I Dubuc1, J Costentin, J P Terranova, M C Barnouin, P Soubrié, G Le Fur, W Rostène, P Kitabgi.   

Abstract

The nonpeptide neurotensin (NT) antagonist, SR 48692, was recently shown to inhibit NT binding to the cloned rat and human NT receptor and to antagonize NT effects in a variety of in vitro and in vivo assays. Here, we show that, in contrast to its antagonistic action on NT-induced hypomotility in the rat, SR 48692 failed to antagonize NT-induced hypothermia and analgesia in the mouse and rat. We suggest that these effects might be mediated through a subtype of SR 48692-insensitive NT receptor.

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Year:  1994        PMID： 8075852      PMCID： PMC1910364          DOI： 10.1111/j.1476-5381.1994.tb13077.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN： 0007-1188            Impact factor:   8.739


  6 in total

1.  Pharmacological effects produced by intracerebral injection of drugs in the conscious mouse.

Authors:  T J HALEY; W G MCCORMICK
Journal:  Br J Pharmacol Chemother       Date:  1957-03

2.  Structure and functional expression of the cloned rat neurotensin receptor.

Authors:  K Tanaka; M Masu; S Nakanishi
Journal:  Neuron       Date:  1990-06       Impact factor: 17.173

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

Authors:  N R al-Rodhan; E Richelson; J A Gilbert; D J McCormick; K S Kanba; M A Pfenning; A Nelson; E W Larson; T L Yaksh
Journal:  Brain Res       Date:  1991-08-23       Impact factor: 3.252

4.  In vivo and in vitro structure-activity studies with peptide and pseudopeptide neurotensin analogs suggest the existence of distinct central neurotensin receptor subtypes.

Authors:  C Labbé-Jullié; I Dubuc; A Brouard; S Doulut; E Bourdel; D Pelaprat; J Mazella; J Martinez; W Rostène; J Costentin
Journal:  J Pharmacol Exp Ther       Date:  1994-01       Impact factor: 4.030

5.  Cloning and expression of a complementary DNA encoding a high affinity human neurotensin receptor.

Authors:  N Vita; P Laurent; S Lefort; P Chalon; X Dumont; M Kaghad; D Gully; G Le Fur; P Ferrara; D Caput
Journal:  FEBS Lett       Date:  1993-02-08       Impact factor: 4.124

6.  Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor.

Authors:  D Gully; M Canton; R Boigegrain; F Jeanjean; J C Molimard; M Poncelet; C Gueudet; M Heaulme; R Leyris; A Brouard
Journal:  Proc Natl Acad Sci U S A       Date:  1993-01-01       Impact factor: 11.205
  6 in total
  20 in total

1.  In vitro functional evidence of different neurotensin-receptors modulating the motor response of human colonic muscle strips.

Authors:  T Croci; G Aureggi; F Guagnini; L Manara; D Gully; G L Fur; J P Maffrand; S Mukenge; G Ferla; P Ferrara; P Chalon; N Vita
Journal:  Br J Pharmacol       Date:  1999-08       Impact factor: 8.739

Review 2.  The role of neurotensin in central nervous system pathophysiology: what is the evidence?

Authors:  Fannie St-Gelais; Claudia Jomphe; Louis-Eric Trudeau
Journal:  J Psychiatry Neurosci       Date:  2006-07       Impact factor: 6.186

Review 3.  Neurotensin agonists: potential in the treatment of schizophrenia.

Authors:  Mona Boules; Amanda Shaw; Paul Fredrickson; Elliott Richelson
Journal:  CNS Drugs       Date:  2007       Impact factor: 5.749

4.  Antagonism by SR 48692 of mechanical responses to neurotensin in rat intestine.

Authors:  F Mulè; R Serio; A Postorino; T Vetri; F Bonvissuto
Journal:  Br J Pharmacol       Date:  1996-02       Impact factor: 8.739

5.  Identification of the receptor subtype involved in the analgesic effect of neurotensin.

Authors:  I Dubuc; P Sarret; C Labbé-Jullié; J M Botto; E Honoré; E Bourdel; J Martinez; J Costentin; J P Vincent; P Kitabgi; J Mazella
Journal:  J Neurosci       Date:  1999-01-01       Impact factor: 6.167

6.  Mediation by neurotensin-receptors of effects of neurotensin on self-stimulation of the medial prefrontal cortex.

Authors:  R Fernández; R Sabater; J A Sáez; R Montes; F Alba; J M Ferrer
Journal:  Br J Pharmacol       Date:  1996-09       Impact factor: 8.739

7.  Central neurotensin receptor activation produces differential behavioral responses in Fischer and Lewis rats.

Authors:  Pat Bauco; Pierre-Paul Rompré
Journal:  Psychopharmacology (Berl)       Date:  2003-04-08       Impact factor: 4.530

8.  Neurotensin inhibition of GABAergic transmission via mGluR-induced endocannabinoid signalling in rat periaqueductal grey.

Authors:  V A Mitchell; H Kawahara; C W Vaughan
Journal:  J Physiol       Date:  2009-04-09       Impact factor: 5.182

9.  Characterization of the effect of SR48692 on inositol monophosphate, cyclic GMP and cyclic AMP responses linked to neurotensin receptor activation in neuronal and non-neuronal cells.

Authors:  F Oury-Donat; O Thurneyssen; N Gonalons; P Forgez; D Gully; G Le Fur; P Soubrie
Journal:  Br J Pharmacol       Date:  1995-09       Impact factor: 8.739

10.  Evidence for a role of NTS2 receptors in the modulation of tonic pain sensitivity.

Authors:  Geneviève Roussy; Marc-André Dansereau; Stéphanie Baudisson; Faouzi Ezzoubaa; Karine Belleville; Nicolas Beaudet; Jean Martinez; Elliott Richelson; Philippe Sarret
Journal:  Mol Pain       Date:  2009-07-06       Impact factor: 3.395
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