SR-142,948
From Wikipedia, the free encyclopedia
 |
|
|---|---|
| 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 | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 184162-64-9 |
| ATC code | ? |
| PubChem | CID 5311451 |
| IUPHAR ligand | 1580 |
| ChemSpider | 4470937  |
| Chemical data | |
| Formula | C39H51N5O6 |
| Mol. mass | 685.850 g/mol |
|
|
|
|
 (what is this?) (verify) |
|
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]
[edit] References
- ^ 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. doi:10.1016/S0306-4522(98)00084-0. PMID 9692718.
- ^ 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. doi:10.1046/j.1460-9568.1999.00506.x. PMID 10103090.
- ^ 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. doi:10.1046/j.1471-4159.2002.00822.x. PMID 12064480.
- ^ 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.
- ^ 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 30 (5): 871–9. doi:10.1038/sj.npp.1300638. PMID 15637639.
- ^ 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. doi:10.1046/j.1460-9568.2003.02859.x. PMID 12956723.
- ^ 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. PMC 2697967. PMID 17675102.
- ^ 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.
- ^ 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.
 |
This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it. |
