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SR-142,948
Systematic (IUPAC) name
2-([5-(2,6-dimethoxyphenyl)-1-[4-[3-(dimethylamino)propyl-methylcarbamoyl]-2-propan-2-ylphenyl]pyrazole-3-carbonyl]amino)adamantane-2-carboxylic acid
Identifiers
CAS number 184162-64-9
ATC code  ?
PubChem 5311451
Chemical data
Formula C 39H51N5O6  
Mol. mass 685.850 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

SR-142,948 is a drug used in scientific research which is a non-peptide antagonist selective for the neurotensin receptors, although not selective between subtypes.[1] It has been used to study the role of neurotensin in the regulation of dopamine receptor activity[2][3][4][5] and glutamate signalling in the brain,[6][7] and in animal studies SR-142,948 blocked the effects of stimulant drugs,[8] including MDMA.[9]

References

  1. ^ Nalivaiko E, Michaud JC, Soubrié P, Le Fur G (October 1998). "Electrophysiological evidence for putative subtypes of neurotensin receptors in guinea-pig mesencephalic dopaminergic neurons". Neuroscience 86 (3): 799–811. PMID 9692718. http://linkinghub.elsevier.com/retrieve/pii/S0306-4522(98)00084-0.  
  2. ^ Alonso R, Gnanadicom H, Fréchin N, Fournier M, Le Fur G, Soubrié P (March 1999). "Blockade of neurotensin receptors suppresses the dopamine D1/D2 synergism on immediate early gene expression in the rat brain". The European Journal of Neuroscience 11 (3): 967–74. PMID 10103090. http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0953-816X&date=1999&volume=11&issue=3&spage=967.  
  3. ^ Matsuyama S, Higashi H, Maeda H, Greengard P, Nishi A (April 2002). "Neurotensin regulates DARPP-32 thr34 phosphorylation in neostriatal neurons by activation of dopamine D1-type receptors". Journal of Neurochemistry 81 (2): 325–34. PMID 12064480. http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0022-3042&date=2002&volume=81&issue=2&spage=325.  
  4. ^ Leonetti M, Brun P, Sotty F, Steinberg R, Soubrié P, Bert L, Renaud B, Suaud-Chagny MF (June 2002). "The neurotensin receptor antagonist SR 142948A blocks the efflux of dopamine evoked in nucleus accumbens by neurotensin ejection into the ventral tegmental area". Naunyn-Schmiedeberg's Archives of Pharmacology 365 (6): 427–33. doi:10.1007/s00210-002-0574-6. PMID 12070755.  
  5. ^ Panayi F, Colussi-Mas J, Lambás-Señas L, Renaud B, Scarna H, Bérod A (May 2005). "Endogenous neurotensin in the ventral tegmental area contributes to amphetamine behavioral sensitization". Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology 30 (5): 871–9. doi:10.1038/sj.npp.1300638. PMID 15637639.  
  6. ^ Matsuyama S, Fukui R, Higashi H, Nishi A (September 2003). "Regulation of DARPP-32 Thr75 phosphorylation by neurotensin in neostriatal neurons: involvement of glutamate signalling". The European Journal of Neuroscience 18 (5): 1247–53. PMID 12956723. http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0953-816X&date=2003&volume=18&issue=5&spage=1247.  
  7. ^ Yin HH, Adermark L, Lovinger DM (January 2008). "Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling". Neuropharmacology 54 (1): 79–86. doi:10.1016/j.neuropharm.2007.06.004. PMID 17675102.  
  8. ^ Reynolds SM, Geisler S, Bérod A, Zahm DS (July 2006). "Neurotensin antagonist acutely and robustly attenuates locomotion that accompanies stimulation of a neurotensin-containing pathway from rostrobasal forebrain to the ventral tegmental area". The European Journal of Neuroscience 24 (1): 188–96. doi:10.1111/j.1460-9568.2006.04791.x. PMID 16882016.  
  9. ^ Marie-Claire C, Palminteri S, Romualdi P, Noble F (June 2008). "Effects of the selective neurotensin antagonist SR 142948A on 3,4-methylenedioxymethamphetamine-induced behaviours in mice". Neuropharmacology 54 (7): 1107–11. doi:10.1016/j.neuropharm.2008.03.001. PMID 18410947.  
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