SR-142,948

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	5311451
ChemSpider	4470937
Hemijski podaci
Formula	C39H51N5O6
Mol. masa	685.850 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C39H51N5O6/c1-23(2)29-21-26(37(46)43(5)15-9-14-42(3)4)12-13-31(29)44-32(35-33(49-6)10-8-11-34(35)50-7)22-30(41-44)36(45)40-39(38(47)48)27-17-24-16-25(19-27)20-28(39)18-24/h8,10-13,21-25,27-28H,9,14-20H2,1-7H3,(H,40,45)(H,47,48) ; Key: LWULHXVBLMWCHO-UHFFFAOYSA-N
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

↑ 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. edit
↑ 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.
↑ 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. edit
↑ 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. ^{[mrtav link]}
↑ 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. ^{[mrtav link]}
↑ 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 : Official Publication of the American College of 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. ^{[mrtav link]}
↑ 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.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Šablon:Neuropeptidni ligandi

[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. 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. edit

[pmid9692718-4] 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.

[pmid10103090-5] 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. ^{[mrtav link]}

[pmid12064480-6] 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. ^{[mrtav link]}

[pmid12070755-7] 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.

[pmid15637639-8] 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.

[pmid12956723-9] 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. ^{[mrtav link]}

[pmid17675102-10] 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.

[pmid16882016-11] 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.

[pmid18410947-12] 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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