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
Identifikatori
CAS broj	184162-64-9
PubChem	CID 5311451
IUPHAR/BPS	1580
ChemSpider	4470937
Hemijski podaci
Formula	C39H51N5O6
Molarna masa	685.850 g/mol
	SMILES O=C(O)C6(NC(=O)c2nn(c1c(cc(C(=O)N(CCCN(C)C)C)cc1)C(C)C)c(c2)c3c(OC)cccc3OC)C4CC5CC6CC(C4)C5; ;
	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 ;

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.^[1] On je korišten u izučavanju uloge neurotenzina u regulaciji aktivnosti dopaminskog receptora^[2]^[3]^[4]^[5] i glutamatne signalizacije u mozgu.^[6]^[7] U životinjskim studies SR-142,948 blokira efekte stimulanata,^[8] kao što je MDMA.^[9]

Reference

^ Nalivaiko E, Michaud JC, Soubrié P, Le Fur G (1998). „Electrophysiological evidence for putative subtypes of neurotensin receptors in guinea-pig mesencephalic dopaminergic neurons”. Neuroscience. 86 (3): 799—811. PMID 9692718. doi:10.1016/S0306-4522(98)00084-0.
^ Alonso R, Gnanadicom H, Fréchin N, Fournier M, Le Fur G, Soubrié P (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. PMID 10103090. doi:10.1046/j.1460-9568.1999.00506.x. ^{[мртва веза]}
^ Matsuyama S, Higashi H, Maeda H, Greengard P, Nishi A (2002). „Neurotensin regulates DARPP-32 thr34 phosphorylation in neostriatal neurons by activation of dopamine D1-type receptors”. Journal of Neurochemistry. 81 (2): 325—34. PMID 12064480. doi:10.1046/j.1471-4159.2002.00822.x. ^{[мртва веза]}
^ Leonetti M, Brun P, Sotty F, Steinberg R, Soubrié P, Bert L, Renaud B, Suaud-Chagny MF (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. PMID 12070755. doi:10.1007/s00210-002-0574-6.
^ Panayi F, Colussi-Mas J, Lambás-Señas L, Renaud B, Scarna H, Bérod A (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. PMID 15637639. doi:10.1038/sj.npp.1300638.
^ Matsuyama S, Fukui R, Higashi H, Nishi A (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. PMID 12956723. doi:10.1046/j.1460-9568.2003.02859.x. ^{[мртва веза]}
^ Yin HH, Adermark L, Lovinger DM (2008). „Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling”. Neuropharmacology. 54 (1): 79—86. PMC 2697967 . PMID 17675102. doi:10.1016/j.neuropharm.2007.06.004.
^ Reynolds SM, Geisler S, Bérod A, Zahm DS (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. PMID 16882016. doi:10.1111/j.1460-9568.2006.04791.x.
^ Marie-Claire C, Palminteri S, Romualdi P, Noble F (2008). „Effects of the selective neurotensin antagonist SR 142948A on 3,4-methylenedioxymethamphetamine-induced behaviours in mice”. Neuropharmacology. 54 (7): 1107—11. PMID 18410947. doi:10.1016/j.neuropharm.2008.03.001.

Spoljašnje veze

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[pmid9692718-1] Nalivaiko E, Michaud JC, Soubrié P, Le Fur G (1998). „Electrophysiological evidence for putative subtypes of neurotensin receptors in guinea-pig mesencephalic dopaminergic neurons”. Neuroscience. 86 (3): 799—811. PMID 9692718. doi:10.1016/S0306-4522(98)00084-0.

[pmid10103090-2] Alonso R, Gnanadicom H, Fréchin N, Fournier M, Le Fur G, Soubrié P (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. PMID 10103090. doi:10.1046/j.1460-9568.1999.00506.x. ^{[мртва веза]}

[pmid12064480-3] Matsuyama S, Higashi H, Maeda H, Greengard P, Nishi A (2002). „Neurotensin regulates DARPP-32 thr34 phosphorylation in neostriatal neurons by activation of dopamine D1-type receptors”. Journal of Neurochemistry. 81 (2): 325—34. PMID 12064480. doi:10.1046/j.1471-4159.2002.00822.x. ^{[мртва веза]}

[pmid12070755-4] Leonetti M, Brun P, Sotty F, Steinberg R, Soubrié P, Bert L, Renaud B, Suaud-Chagny MF (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. PMID 12070755. doi:10.1007/s00210-002-0574-6.

[pmid15637639-5] Panayi F, Colussi-Mas J, Lambás-Señas L, Renaud B, Scarna H, Bérod A (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. PMID 15637639. doi:10.1038/sj.npp.1300638.

[pmid12956723-6] Matsuyama S, Fukui R, Higashi H, Nishi A (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. PMID 12956723. doi:10.1046/j.1460-9568.2003.02859.x. ^{[мртва веза]}

[pmid17675102-7] Yin HH, Adermark L, Lovinger DM (2008). „Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling”. Neuropharmacology. 54 (1): 79—86. PMC 2697967 . PMID 17675102. doi:10.1016/j.neuropharm.2007.06.004.

[pmid16882016-8] Reynolds SM, Geisler S, Bérod A, Zahm DS (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. PMID 16882016. doi:10.1111/j.1460-9568.2006.04791.x.

[pmid18410947-9] Marie-Claire C, Palminteri S, Romualdi P, Noble F (2008). „Effects of the selective neurotensin antagonist SR 142948A on 3,4-methylenedioxymethamphetamine-induced behaviours in mice”. Neuropharmacology. 54 (7): 1107—11. PMID 18410947. doi:10.1016/j.neuropharm.2008.03.001.

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