104632-28-2

• 常用中文名：(R)-普拉克索
• 常用英文名：Dexpramipexole
• CAS号：104632-28-2
• 分子式：C₁₀H₁₇N₃S
• 分子量：211.331
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 多巴胺受体
• 发布时间：2018-09-18 18:40:47
• 更新时间：2024-01-02 11:11:29
• Dexpramipexole(KNS-760704)也叫R-(+)-Pramipexole,是神经保护剂,是弱的非麦角类多巴胺受体激动剂。

名称

• 中文名: R-普拉克索
• 英文名: (6R)-6-N-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine
• 中文别名: (R)-普拉克索二盐酸化物; (R)-普拉克索; 普拉克索杂质E
• 英文别名: Dexpramipexole; (6R)-2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole; (R)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine; (6R)-4,5,6,7-tetrahydro-N6-propylbenzothiazole-2,6-diamine; (R)-Pramipexole Dihydrochloride; Pramipexole [USAN:INN]; (R)-(+)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole; (R)-Pramipexole; (R)-(+)-pramipexole

物化性质

• 密度: 1.17±0.1 g/cm3
• 熔点: 270-272ºC
• 分子式: C₁₀H₁₇N₃S
• 分子量: 211.331
• PSA: 83.52000
• LogP: 4.38490
• 储存条件: 室温，干燥，密封
• 水溶解性: Slightly soluble (1.1 g/L) (25 ºC)

生物活性

• 描述: Dexpramipexole(KNS-760704)也叫R-(+)-Pramipexole,是神经保护剂,是弱的非麦角类多巴胺受体激动剂。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体
  信号通路 >> 神经信号通路 >> 多巴胺受体
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Rudnicki SA, Berry JD, Ingersoll E, et al. Dexpramipexole effects on functional decline and survival in subjects with amyotrophic lateral sclerosis in a Phase II study: subgroup analysis of demographic and clinical characteristics. Amyotroph Lateral Scler

  [2]. Alavian KN, Dworetzky SI, Bonanni L, et al. Effects of dexpramipexole on brain mitochondrial conductances and cellular bioenergetic efficiency. Brain Res. 2012 Mar 29;1446:1-11.

  [3]. Cudkowicz M, Bozik ME, Ingersoll EW, et al. The effects of dexpramipexole (KNS-760704) in individuals with amyotrophic lateral sclerosis. Nat Med. 2011 Nov 20;17(12):1652-6.

  [4]. Bozik ME, Mather JL, Kramer WG, et al. Safety, tolerability, and pharmacokinetics of KNS-760704 (dexpramipexole) in healthy adult subjects. J Clin Pharmacol. 2011 Aug;51(8):1177-85.

  [5]. Cheah BC, Kiernan MC. Dexpramipexole, the R(+) enantiomer of pramipexole, for the potential treatment of amyotrophic lateral sclerosis. IDrugs. 2010 Dec;13(12):911-20.

安全

• 危害码 (欧洲): Xi
• 海关编码: 2934999090

合成路线

1332723-78-0 ~% 104632-28-2

文献：WO2013/96816 A1, ; Paragraph 000145-000146 ;

106006-85-3 ~% 104632-28-2

文献：Journal of Medicinal Chemistry, , vol. 30, # 3 p. 494 - 498

147-71-7 104617-86-9 ~% 104632-28-2 104632-26-0

文献：WO2010/22140 A1, ; Page/Page column 100-101 ;

106092-11-9 ~% 104632-28-2

文献：Journal of Medicinal Chemistry, , vol. 30, # 3 p. 494 - 498

106006-83-1 ~% 104632-28-2

文献：Journal of Medicinal Chemistry, , vol. 30, # 3 p. 494 - 498

104617-86-9 ~0% 104632-28-2 104632-26-0

文献：GENERICS [UK] LIMITED Patent: WO2006/3471 A2, 2006 ; Location in patent: Page/Page column 9-11 ;

上下游产品

上游产品  5
106006-85-3 147-71-7 104617-86-9 106092-11-9
106006-83-1
下游产品  0

海关

海关编码	2934999090
中文概述	2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素	品名, 成分含量, 用途
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%