| 描述 |
盐酸伏诺哌嗪是一种质子泵抑制剂(PPI),是一种有效的口服活性钾竞争性酸阻滞剂(P-CAB),具有抗分泌活性。盐酸伏诺哌嗪在pH 6.5时抑制猪胃微粒体中的H+,K+-ATP酶活性,IC50为19 nM。盐酸伏诺哌嗪用于研究酸相关疾病,如胃食管反流病和消化性溃疡病。盐酸沃诺哌嗪可用于根除幽门螺杆菌[1][2][3]。
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| 相关类别 |
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| 靶点 |
IC50: 19 nM (porcine gastric H+,K+-ATPase, at pH 6.5)[2]
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| 体外研究 |
伏诺哌嗪(0.1 nM-10μM；30分钟)以浓度依赖性方式显示猪胃H+,K+-ATP酶活性[2]。伏诺哌嗪不抑制Na+,K+-ATP酶活性,即使其浓度比其对胃H+,K+-ATP酶的IC50值高500倍[2]。
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| 体内研究 |
在4 mg/kg剂量下,伏诺哌嗪(1-4 mg/kg；p.o.)完全抑制大鼠基础和2-脱氧-D-葡萄糖(200 mg/kg；s.c.)刺激的胃酸分泌[2]。动物模型：7或8周龄雄性Sprague-Dawley大鼠[2]剂量：0.5 mg/kg、1 mg/kg,2 mg/kg和4 mg/kg给药：口服给药结果：以剂量依赖性方式抑制基础胃酸分泌。
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| 参考文献 |
[1]. Arikawa Y, et al. Discovery of a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB). J Med Chem, 2012, 55(9), 4446-4456. [2]. Hori Y, et al. 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438), a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases. J Pharmacol Exp Ther, 2010, 335(1), 231-238. [3]. Sugimoto M, et al. Role of Vonoprazan in Helicobacter pylori Eradication Therapy in Japan. Front Pharmacol. 2019 Jan 15;9:1560.
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