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编 号：F230643
分子式：C18H24ClFN2O2
分子量：354.85
分子式：C18H24ClFN2O2
分子量：354.85
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CAS No: 184674-99-5
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生物活性：
Robalzotan hydrochloride (NAD-?299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system.
体内研究：
Robalzotan hydrochloride (1-100 μg/kg；i.v.) 在大鼠体内以 5 μg/kg 显着增加此类神经元的活性，并逆转 citalopram (HY-121203) (300 μg/kg i.v.) 或 paroxetine (HY-122272) (100 μg/kg， i.v.) 对大鼠中缝背核 5-HT神经元活性的影响.Robalzotan hydrochloride (5, 50 μg/kg；静脉注射) 提高 5-HT 细胞的放电率。Robalzotan hydrochloride (2-100 μg/kg; i.v.) 在猴子体内以剂量依赖性方式占据 5-HT1A 受体。Robalzotan hydrochloride (0.3；1 和 3 μmol/kg 皮下注射) 引起大鼠 FC 细胞外 ACh 水平的剂量依赖性增加。Animal Model:300-600 g, male Sprague-Dawley rats (5-HT cells)
Dosage:1, 5, 12.5, 25, 50, 100 μg/kg
Administration:I.v.
Result:Significantly increased the activity of such neurons at 5 μg/kg, increasing doses of robalzotan 5-100 μg/kg or 50-400 mg/kg did not further affect the firing rate of 5-HT neurons.
Animal Model:3-4 kg, cynomolgus monkeys
Dosage:2, 10, 20, 100 μg/kg
Administration:I.v.
Result:Occupied 5-HT1A receptors in a dose-dependent and saturable manner and he highest 5-HT1A receptor occupancy (70-80%) was attained after 100 μg/kg.
Robalzotan hydrochloride (NAD-?299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system.
体内研究：
Robalzotan hydrochloride (1-100 μg/kg；i.v.) 在大鼠体内以 5 μg/kg 显着增加此类神经元的活性，并逆转 citalopram (HY-121203) (300 μg/kg i.v.) 或 paroxetine (HY-122272) (100 μg/kg， i.v.) 对大鼠中缝背核 5-HT神经元活性的影响.Robalzotan hydrochloride (5, 50 μg/kg；静脉注射) 提高 5-HT 细胞的放电率。Robalzotan hydrochloride (2-100 μg/kg; i.v.) 在猴子体内以剂量依赖性方式占据 5-HT1A 受体。Robalzotan hydrochloride (0.3；1 和 3 μmol/kg 皮下注射) 引起大鼠 FC 细胞外 ACh 水平的剂量依赖性增加。Animal Model:300-600 g, male Sprague-Dawley rats (5-HT cells)
Dosage:1, 5, 12.5, 25, 50, 100 μg/kg
Administration:I.v.
Result:Significantly increased the activity of such neurons at 5 μg/kg, increasing doses of robalzotan 5-100 μg/kg or 50-400 mg/kg did not further affect the firing rate of 5-HT neurons.
Animal Model:3-4 kg, cynomolgus monkeys
Dosage:2, 10, 20, 100 μg/kg
Administration:I.v.
Result:Occupied 5-HT1A receptors in a dose-dependent and saturable manner and he highest 5-HT1A receptor occupancy (70-80%) was attained after 100 μg/kg.
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