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编 号：F746055
分子式：C22H26F2N4O2
分子量：416.46
分子式：C22H26F2N4O2
分子量：416.46
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CAS No: 1609342-18-8
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生物活性：
BAY-747 (BAY 1165747) is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model.
体内研究：
BAY-747 在研究的时间范围内显示出 0.6 ± 2.0 的脑血浆比，反映出 60% 的相对较高的脑渗透。BAY-747（0.03-1.0 mg/kg，2 mL/kg；口服；在 24 小时间隔 OLT 中 T1 前 30 分钟）增强大鼠对象定位任务 (OLT) 模型中的长期记忆获取过程，并减弱 L -NAME 引起短期记忆障碍。 BAY-747 不影响海马体中含有 GluA1 的 AMPAR 动力学。BAY-747（0.003-0.3 mg/kg；口服；单剂量）降低大鼠的血压，并且（3 mg/kg；口服；每天一次，持续 35 天）增加接受 l-NAME 处理的肾素的大鼠体重 转基因模型。BAY-747（150 mg/kg 食物；口服；16 周）提高雄性 mdx/mTRG2 小鼠的握力和跑步速度，表明骨骼肌功能得到改善。Animal Model:Rat object location task (OLT) model
Dosage:0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration:PO; 30 min before T1 in a 24 h interval OLT
Result:Resulted significantly higher long-term memory performance at 0.03, 0.1, 0.3 and 1.0 mg/kg dose, 30 min before T1. Attenuated L-NAME induced short-term memory impairments at 0.3 mg/kg and 1 mg/kg.Did not enhance GluA1 trafficking at 1 mg/kg 24 h after treatment.
Animal Model:Anesthetized, conscious spontaneously hypertensive and conscious normotensive rats
Dosage:0 mg/kg, 0.003 mg/kg, 0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, and 0.3 mg/kg
Administration:IV; single dose
Result:Produced a dose-dependent and long-lasting decrease in blood pressure in rats.
Animal Model:l-NAME-Treated Renin Transgenic Rats
Dosage:0.3 mg/kg, 3 mg/kg
Administration:PO; once daily for 35 days; l-NAME treatment: 30 mg/kg, po, for 6 days
Result:Resulted a significant weight gain among rats.Led to a dose-dependent increase of plasma cGMP. Decreased blood pressure only at 3 mg/kg.
体外研究：
BAY-747 (100 nM) 与 WS 组合使用，可增强体外采集样 cLTP 模型中 AMPA 受体动力学 。
BAY-747 (BAY 1165747) is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model.
体内研究：
BAY-747 在研究的时间范围内显示出 0.6 ± 2.0 的脑血浆比，反映出 60% 的相对较高的脑渗透。BAY-747（0.03-1.0 mg/kg，2 mL/kg；口服；在 24 小时间隔 OLT 中 T1 前 30 分钟）增强大鼠对象定位任务 (OLT) 模型中的长期记忆获取过程，并减弱 L -NAME 引起短期记忆障碍。 BAY-747 不影响海马体中含有 GluA1 的 AMPAR 动力学。BAY-747（0.003-0.3 mg/kg；口服；单剂量）降低大鼠的血压，并且（3 mg/kg；口服；每天一次，持续 35 天）增加接受 l-NAME 处理的肾素的大鼠体重 转基因模型。BAY-747（150 mg/kg 食物；口服；16 周）提高雄性 mdx/mTRG2 小鼠的握力和跑步速度，表明骨骼肌功能得到改善。Animal Model:Rat object location task (OLT) model
Dosage:0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration:PO; 30 min before T1 in a 24 h interval OLT
Result:Resulted significantly higher long-term memory performance at 0.03, 0.1, 0.3 and 1.0 mg/kg dose, 30 min before T1. Attenuated L-NAME induced short-term memory impairments at 0.3 mg/kg and 1 mg/kg.Did not enhance GluA1 trafficking at 1 mg/kg 24 h after treatment.
Animal Model:Anesthetized, conscious spontaneously hypertensive and conscious normotensive rats
Dosage:0 mg/kg, 0.003 mg/kg, 0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, and 0.3 mg/kg
Administration:IV; single dose
Result:Produced a dose-dependent and long-lasting decrease in blood pressure in rats.
Animal Model:l-NAME-Treated Renin Transgenic Rats
Dosage:0.3 mg/kg, 3 mg/kg
Administration:PO; once daily for 35 days; l-NAME treatment: 30 mg/kg, po, for 6 days
Result:Resulted a significant weight gain among rats.Led to a dose-dependent increase of plasma cGMP. Decreased blood pressure only at 3 mg/kg.
体外研究：
BAY-747 (100 nM) 与 WS 组合使用，可增强体外采集样 cLTP 模型中 AMPA 受体动力学 。
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