Chemistry:SR-142948

From HandWiki
Short description: Chemical compound
SR-142948
SR142948 structure.png
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
Chemical and physical data
FormulaC39H51N5O6
Molar mass685.866 g·mol−1
3D model (JSmol)
  (verify)

SR-142948 is a drug used in scientific research which is a non-peptide antagonist selective for the neurotensin receptors, although not selective between subtypes.[1]

Study

SR-142948 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]

In animal studies, SR-142948 blocked the effects of stimulant drugs,[8] including MDMA.[9]

References

  1. "Electrophysiological evidence for putative subtypes of neurotensin receptors in guinea-pig mesencephalic dopaminergic neurons". Neuroscience 86 (3): 799–811. October 1998. doi:10.1016/S0306-4522(98)00084-0. PMID 9692718. 
  2. "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. March 1999. doi:10.1046/j.1460-9568.1999.00506.x. PMID 10103090. 
  3. "Neurotensin regulates DARPP-32 thr34 phosphorylation in neostriatal neurons by activation of dopamine D1-type receptors". Journal of Neurochemistry 81 (2): 325–34. April 2002. doi:10.1046/j.1471-4159.2002.00822.x. PMID 12064480. 
  4. "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. June 2002. doi:10.1007/s00210-002-0574-6. PMID 12070755. 
  5. "Endogenous neurotensin in the ventral tegmental area contributes to amphetamine behavioral sensitization". Neuropsychopharmacology 30 (5): 871–9. May 2005. doi:10.1038/sj.npp.1300638. PMID 15637639. 
  6. "Regulation of DARPP-32 Thr75 phosphorylation by neurotensin in neostriatal neurons: involvement of glutamate signalling". The European Journal of Neuroscience 18 (5): 1247–53. September 2003. doi:10.1046/j.1460-9568.2003.02859.x. PMID 12956723. 
  7. "Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling". Neuropharmacology 54 (1): 79–86. January 2008. doi:10.1016/j.neuropharm.2007.06.004. PMID 17675102. 
  8. "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. July 2006. doi:10.1111/j.1460-9568.2006.04791.x. PMID 16882016. 
  9. "Effects of the selective neurotensin antagonist SR 142948A on 3,4-methylenedioxymethamphetamine-induced behaviours in mice". Neuropharmacology 54 (7): 1107–11. June 2008. doi:10.1016/j.neuropharm.2008.03.001. PMID 18410947. http://www.hal.inserm.fr/inserm-00278426/document.