SR-142948

SR-142948
IUPAC命名法による物質名
	IUPAC名 2-([5-(2,6-dimethoxyphenyl)-1-[4-[3-(dimethylamino)propyl-methylcarbamoyl]-2-propan-2-ylphenyl]pyrazole-3-carbonyl]amino)adamantane-2-carboxylic acid;
データベースID
CAS番号;	184162-64-9
PubChem	CID: 5311451
IUPHAR/BPS（英語版）	1580
ChemSpider	4470937
化学的データ
化学式	C39H51N5O6
分子量	685.87 g·mol−1
	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 ;
	テンプレートを表示

SR-142948は、科学研究で使用される薬品である。非ペプチド性ニューロテンシン受容体選択的アンタゴニストであるが、サブタイプ間では選択的ではない^[1]。

研究

主に、ドーパミン受容体活性の調節^[2]^[3]^[4]^[5]や脳内のグルタミン酸シグナル伝達におけるニューロテンシンの役割を研究するために使用される^[6]^[7]。

動物研究ではMDMAなどの覚醒剤の効果を阻害する^[8]^[9]。

出典

^ Nalivaiko E, Michaud JC, Soubrié P, Le Fur G (1998年10月)『Electrophysiological evidence for putative subtypes of neurotensin receptors in guinea-pig mesencephalic dopaminergic neurons』Neuroscience. 86 (3): 799~811頁. doi:10.1016/S0306-4522(98)00084-0. PMID 9692718.
^ Alonso R, Gnanadicom H, Fréchin N, Fournier M, Le Fur G, Soubrié P (1999年3月)『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): 967~974頁. doi:10.1046/j.1460-9568.1999.00506.x. PMID 10103090.
^ Matsuyama S, Higashi H, Maeda H, Greengard P, Nishi A (2002年4月)『Neurotensin regulates DARPP-32 thr34 phosphorylation in neostriatal neurons by activation of dopamine D1-type receptors』Journal of Neurochemistry. 81 (2): 325~334頁. doi:10.1046/j.1471-4159.2002.00822.x. PMID 12064480.
^ Leonetti M, Brun P, Sotty F, Steinberg R, Soubrié P, Bert L, et al. (2002年6月)『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): 427~433頁. doi:10.1007/s00210-002-0574-6. PMID 12070755.
^ Panayi F, Colussi-Mas J, Lambás-Señas L, Renaud B, Scarna H, Bérod A (2005年5月)『Endogenous neurotensin in the ventral tegmental area contributes to amphetamine behavioral sensitization』Neuropsychopharmacology. 30 (5): 871~879頁. doi:10.1038/sj.npp.1300638. PMID 15637639.
^ Matsuyama S, Fukui R, Higashi H, Nishi A (2003年9月)『Regulation of DARPP-32 Thr75 phosphorylation by neurotensin in neostriatal neurons: involvement of glutamate signalling』The European Journal of Neuroscience. 18 (5): 1247~1253頁. doi:10.1046/j.1460-9568.2003.02859.x. PMID 12956723.
^ Yin HH, Adermark L, Lovinger DM (2008年1月). "Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling". Neuropharmacology. 54 (1): 79~86頁. doi:10.1016/j.neuropharm.2007.06.004. PMC 2697967. PMID 17675102.
^ Reynolds SM, Geisler S, Bérod A, Zahm DS (2006年7月)『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): 188~196頁. doi:10.1111/j.1460-9568.2006.04791.x. PMID 16882016.
^ Marie-Claire C, Palminteri S, Romualdi P, Noble F (2008年6月)『Effects of the selective neurotensin antagonist SR 142948A on 3,4-methylenedioxymethamphetamine-induced behaviours in mice』Neuropharmacology. 54 (7): 1107~1111頁. doi:10.1016/j.neuropharm.2008.03.001. PMID 18410947.

[1] Nalivaiko E, Michaud JC, Soubrié P, Le Fur G (1998年10月)『Electrophysiological evidence for putative subtypes of neurotensin receptors in guinea-pig mesencephalic dopaminergic neurons』Neuroscience. 86 (3): 799~811頁. doi:10.1016/S0306-4522(98)00084-0. PMID 9692718.

[2] Alonso R, Gnanadicom H, Fréchin N, Fournier M, Le Fur G, Soubrié P (1999年3月)『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): 967~974頁. doi:10.1046/j.1460-9568.1999.00506.x. PMID 10103090.

[3] Matsuyama S, Higashi H, Maeda H, Greengard P, Nishi A (2002年4月)『Neurotensin regulates DARPP-32 thr34 phosphorylation in neostriatal neurons by activation of dopamine D1-type receptors』Journal of Neurochemistry. 81 (2): 325~334頁. doi:10.1046/j.1471-4159.2002.00822.x. PMID 12064480.

[4] Leonetti M, Brun P, Sotty F, Steinberg R, Soubrié P, Bert L, et al. (2002年6月)『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): 427~433頁. doi:10.1007/s00210-002-0574-6. PMID 12070755.

[5] Panayi F, Colussi-Mas J, Lambás-Señas L, Renaud B, Scarna H, Bérod A (2005年5月)『Endogenous neurotensin in the ventral tegmental area contributes to amphetamine behavioral sensitization』Neuropsychopharmacology. 30 (5): 871~879頁. doi:10.1038/sj.npp.1300638. PMID 15637639.

[6] Matsuyama S, Fukui R, Higashi H, Nishi A (2003年9月)『Regulation of DARPP-32 Thr75 phosphorylation by neurotensin in neostriatal neurons: involvement of glutamate signalling』The European Journal of Neuroscience. 18 (5): 1247~1253頁. doi:10.1046/j.1460-9568.2003.02859.x. PMID 12956723.

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

[8] Reynolds SM, Geisler S, Bérod A, Zahm DS (2006年7月)『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): 188~196頁. doi:10.1111/j.1460-9568.2006.04791.x. PMID 16882016.

[9] Marie-Claire C, Palminteri S, Romualdi P, Noble F (2008年6月)『Effects of the selective neurotensin antagonist SR 142948A on 3,4-methylenedioxymethamphetamine-induced behaviours in mice』Neuropharmacology. 54 (7): 1107~1111頁. doi:10.1016/j.neuropharm.2008.03.001. PMID 18410947.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]