SR-142,948

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SR-142,948
(IUPAC) ime
2-([5-(2,6-dimethoxyphenyl)-1-[4-[3-(dimethylamino)propyl-methylcarbamoyl]-2-propan-2-ylphenyl]pyrazole-3-carbonyl]amino)adamantane-2-carboxylic acid
Klinički podaci
Identifikatori
CAS broj 184162-64-9
ATC kod ?
PubChem[1][2] 5311451
ChemSpider[3] 4470937
Hemijski podaci
Formula C39H51N5O6 
Mol. masa 685.850 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

SR-142,948 je lek koji se koristi u naučnim istraživanjima. On pripada grupi nepeptidnih antagonista selektivnih za neurotenzinske receptore, mada nije selektivan za specifični tip tog receptora.[4] On je korišten u izučavanju uloge neurotenzina u regulaciji aktivnosti dopaminskog receptora[5][6][7][8] i glutamatne signalizacije u mozgu.[9][10] U životinjskim studies SR-142,948 blokira efekte stimulanata,[11] kao što je MDMA.[12]

Reference[uredi - уреди | uredi kôd]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. http://www.sciencedirect.com/science/article/pii/S1359644610007737.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. http://www.jcheminf.com/content/2/1/3.  edit
  4. 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. http://linkinghub.elsevier.com/retrieve/pii/S0306-4522(98)00084-0. 
  5. 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. http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0953-816X&date=1999&volume=11&issue=3&spage=967. [mrtav link]
  6. 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. http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0022-3042&date=2002&volume=81&issue=2&spage=325. [mrtav link]
  7. 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. 
  8. 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. 
  9. 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. http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0953-816X&date=2003&volume=18&issue=5&spage=1247. [mrtav link]
  10. 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. //www.ncbi.nlm.nih.gov/pmc/articles/PMC2697967/. 
  11. 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. 
  12. 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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Šablon:Neuropeptidni ligandi

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