SR-142948 explained

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]

Notes and References

1. Nalivaiko E, Michaud JC, Soubrié P, Le Fur G . Electrophysiological evidence for putative subtypes of neurotensin receptors in guinea-pig mesencephalic dopaminergic neurons . Neuroscience . 86 . 3 . 799–811 . October 1998 . 9692718 . 10.1016/S0306-4522(98)00084-0 . 41883743 .
2. Alonso R, Gnanadicom H, Fréchin N, Fournier M, Le Fur G, Soubrié P . 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 . 10103090 . 10.1046/j.1460-9568.1999.00506.x . 9622032 .
3. Matsuyama S, Higashi H, Maeda H, Greengard P, Nishi A . 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 . 12064480 . 10.1046/j.1471-4159.2002.00822.x . 31073155 .
4. Leonetti M, Brun P, Sotty F, Steinberg R, Soubrié P, Bert L, Renaud B, Suaud-Chagny MF . 6 . 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 . 12070755 . 10.1007/s00210-002-0574-6 . 2934039 .
5. Panayi F, Colussi-Mas J, Lambás-Señas L, Renaud B, Scarna H, Bérod A . Endogenous neurotensin in the ventral tegmental area contributes to amphetamine behavioral sensitization . Neuropsychopharmacology . 30 . 5 . 871–9 . May 2005 . 15637639 . 10.1038/sj.npp.1300638 . free .
6. Matsuyama S, Fukui R, Higashi H, Nishi A . 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 . 12956723 . 10.1046/j.1460-9568.2003.02859.x . 23999624 .
7. Yin HH, Adermark L, Lovinger DM . Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling . Neuropharmacology . 54 . 1 . 79–86 . January 2008 . 17675102 . 2697967 . 10.1016/j.neuropharm.2007.06.004 .
8. Reynolds SM, Geisler S, Bérod A, Zahm DS . 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 . 16882016 . 10.1111/j.1460-9568.2006.04791.x . 35592039 .
9. Marie-Claire C, Palminteri S, Romualdi P, Noble F . Effects of the selective neurotensin antagonist SR 142948A on 3,4-methylenedioxymethamphetamine-induced behaviours in mice . Neuropharmacology . 54 . 7 . 1107–11 . June 2008 . 18410947 . 10.1016/j.neuropharm.2008.03.001 . 15455279 .