630119-43-6

• 常用中文名：ABT-670
• 常用英文名：ABT-670
• CAS号：630119-43-6
• 分子式：C₁₉H₂₃N₃O₂
• 分子量：325.40500
• 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：2016-09-01 02:18:21
• 更新时间：2024-01-22 11:15:55
• ABT-670是一种具有选择性,可口服的dopamine D4受体抑制剂。

名称

• 中文名: ABT-670
• 英文名: 3-methyl-N-[[4-(1-oxidopyridin-1-ium-2-yl)piperidin-1-yl]methyl]benzamide
• 英文别名: 2-(1-{[(3-methylbenzoyl)amino]methyl}-4-piperidinyl)pyridinium N-oxide; UNII-4L6071XH2J; Benzamide,3-methyl-N-[[4-(1-oxido-2-pyridinyl)-1-piperidinyl]methyl]; ABT-670

物化性质

• 分子式: C₁₉H₂₃N₃O₂
• 分子量: 325.40500
• 精确质量: 325.17900
• PSA: 61.29000
• LogP: 3.50310
• 储存条件: 2-8℃

生物活性

• 描述: ABT-670是一种具有选择性,可口服的dopamine D4受体抑制剂。
• 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 >> 其他
• 靶点:

  EC50: 89 nM (Human D4), 160 nM (Ferret D4), 93 nM (Rat D4)[1]

• 体外研究: ABT-670是一种选择性D4激动剂,对人D4,雪貂D4和大鼠D4的EC50分别为89 nM,160 nM和93 nM [1]。
• 体内研究: ABT-670(0.1μmol/ kg)可强烈诱导雄性大鼠勃起的高发(75％)。 ABT-670在大鼠,狗和猴中表现出优异的口服生物利用度(分别为68％,85％和91％),具有相当的疗效,安全性和耐受性[1]。
• 参考文献:

  [1]. Patel MV, et al. Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction. J Med Chem. 2006 Dec 14;49(25):7450-65.

合成路线

50-00-0 618-47-3 ~% 630119-43-6

文献：Bhatia, Pramila A.; Daanen, Jerome F.; Hakeem, Ahmed A.; Kolasa, Teodozyj; Matulenko, Mark A.; Mortell, Kathleen H.; Patel, Meena V.; Stewart, Andrew O.; Wang, Xueqing; Xia, Zhiren; Zhang, Henry Q. Patent: US2003/229094 A1, 2003 ; Location in patent: Page 98 ; US 20030229094 A1

79099-07-3 ~% 630119-43-6

文献：Patel, Meena V.; Kolasa, Teodozyj; Mortell, Kathleen; Matulenko, Mark A.; Hakeem, Ahmed A.; Rohde, Jeffrey J.; Nelson, Sherry L.; Cowart, Marlon D.; Nakane, Masaki; Miller, Loan N.; Uchic, Marie E.; Terranova, Marc A.; El-Kouhen, Odile F.; Donnelly-Roberts, Diana L.; Namovic, Marian T.; Hollingsworth, Peter R.; Chang, Renjie; Martino, Brenda R.; Wetter, Jill M.; Marsh, Kennan C.; Martin, Ruth; Darbyshire, John F.; Gintant, Gary; Hsieh, Gin C.; Moreland, Robert B.; Sullivan, James P.; Brioni, Jorge D.; Stewart, Andrew O. Journal of Medicinal Chemistry, 2006 , vol. 49, # 25 p. 7450 - 7465

138647-49-1 ~% 630119-43-6

文献：Patel, Meena V.; Kolasa, Teodozyj; Mortell, Kathleen; Matulenko, Mark A.; Hakeem, Ahmed A.; Rohde, Jeffrey J.; Nelson, Sherry L.; Cowart, Marlon D.; Nakane, Masaki; Miller, Loan N.; Uchic, Marie E.; Terranova, Marc A.; El-Kouhen, Odile F.; Donnelly-Roberts, Diana L.; Namovic, Marian T.; Hollingsworth, Peter R.; Chang, Renjie; Martino, Brenda R.; Wetter, Jill M.; Marsh, Kennan C.; Martin, Ruth; Darbyshire, John F.; Gintant, Gary; Hsieh, Gin C.; Moreland, Robert B.; Sullivan, James P.; Brioni, Jorge D.; Stewart, Andrew O. Journal of Medicinal Chemistry, 2006 , vol. 49, # 25 p. 7450 - 7465

90606-77-2 ~% 630119-43-6

文献：Patel, Meena V.; Kolasa, Teodozyj; Mortell, Kathleen; Matulenko, Mark A.; Hakeem, Ahmed A.; Rohde, Jeffrey J.; Nelson, Sherry L.; Cowart, Marlon D.; Nakane, Masaki; Miller, Loan N.; Uchic, Marie E.; Terranova, Marc A.; El-Kouhen, Odile F.; Donnelly-Roberts, Diana L.; Namovic, Marian T.; Hollingsworth, Peter R.; Chang, Renjie; Martino, Brenda R.; Wetter, Jill M.; Marsh, Kennan C.; Martin, Ruth; Darbyshire, John F.; Gintant, Gary; Hsieh, Gin C.; Moreland, Robert B.; Sullivan, James P.; Brioni, Jorge D.; Stewart, Andrew O. Journal of Medicinal Chemistry, 2006 , vol. 49, # 25 p. 7450 - 7465

279250-32-7 ~% 630119-43-6

文献：Patel, Meena V.; Kolasa, Teodozyj; Mortell, Kathleen; Matulenko, Mark A.; Hakeem, Ahmed A.; Rohde, Jeffrey J.; Nelson, Sherry L.; Cowart, Marlon D.; Nakane, Masaki; Miller, Loan N.; Uchic, Marie E.; Terranova, Marc A.; El-Kouhen, Odile F.; Donnelly-Roberts, Diana L.; Namovic, Marian T.; Hollingsworth, Peter R.; Chang, Renjie; Martino, Brenda R.; Wetter, Jill M.; Marsh, Kennan C.; Martin, Ruth; Darbyshire, John F.; Gintant, Gary; Hsieh, Gin C.; Moreland, Robert B.; Sullivan, James P.; Brioni, Jorge D.; Stewart, Andrew O. Journal of Medicinal Chemistry, 2006 , vol. 49, # 25 p. 7450 - 7465

206446-49-3 ~% 630119-43-6

文献：Patel, Meena V.; Kolasa, Teodozyj; Mortell, Kathleen; Matulenko, Mark A.; Hakeem, Ahmed A.; Rohde, Jeffrey J.; Nelson, Sherry L.; Cowart, Marlon D.; Nakane, Masaki; Miller, Loan N.; Uchic, Marie E.; Terranova, Marc A.; El-Kouhen, Odile F.; Donnelly-Roberts, Diana L.; Namovic, Marian T.; Hollingsworth, Peter R.; Chang, Renjie; Martino, Brenda R.; Wetter, Jill M.; Marsh, Kennan C.; Martin, Ruth; Darbyshire, John F.; Gintant, Gary; Hsieh, Gin C.; Moreland, Robert B.; Sullivan, James P.; Brioni, Jorge D.; Stewart, Andrew O. Journal of Medicinal Chemistry, 2006 , vol. 49, # 25 p. 7450 - 7465