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编 号：F760278
分子式：C20H27NO3
分子量：329.43
分子式：C20H27NO3
分子量：329.43
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CAS No: 778546-51-3
产品详情
生物活性：
A-77636 is an orally active, potent, selective and long-acting dopamine D1 receptor agonist (pEC50 = 8.13; EC50 = 1.1 nM). A-77636 shows the highest affinity (pKi = 7.40 ± 0.09; Ki = 39.8 nM) for the dopamine D1 receptor. A-77636 shows antiparkinsonian activity.
体内研究：
A-77636 (0-3.2 μmol/kg，皮下注射) 在 6-OHDA 损伤的大鼠中引发旋转行为(ED50=0.32 μmol/kg sc)。A-77636 (1-10 mg/kg) 以剂量依赖性方式减弱成瘾剂诱导的运动活动。A-77636 在大鼠 (ED50=12.3 μmol/kg s.c.) 和小鼠 (ED50=12.1 μmol/kg s.c.) 中产生前肢阵挛 。在用 MPTP 处理以诱导帕金森样状态的狨猴中，A-77636 (0.5、1.0 或 2.0 μmol/kg，口服)可增加运动活性并降低帕金森样症状的严重程度：该化合物在皮下或口服给药后均有活性。Animal Model:Rats with unilateral 6-OHDA (6-hydroxydopamine) lesions of the nigrostriatal pathway (six/group)
Dosage:0.32, 1.0, 3.2 μmol/kg
Administration:Subcutaneously
Result:Elicited prolonged (> 20 h) contralateral turning, which was blocked by SCH 23390, a D1 receptor antagonist, but not by haloperidol at doses selective for the dopamine D2 receptor.
Animal Model:Male Swiss Webster mice (18-25 g, five or six per cage)
Dosage:1, 3, 10 mg/kg
Administration:
Result:Attenuated addiction-induced locomotor activity in a dose-dependent manner. When administered alone, 1 and 3 mg/kg A-77636 produced little change in locomotor activity, whereas 10 mg/kg produced a significant and substantial decrease in locomotor activity.
A-77636 is an orally active, potent, selective and long-acting dopamine D1 receptor agonist (pEC50 = 8.13; EC50 = 1.1 nM). A-77636 shows the highest affinity (pKi = 7.40 ± 0.09; Ki = 39.8 nM) for the dopamine D1 receptor. A-77636 shows antiparkinsonian activity.
体内研究：
A-77636 (0-3.2 μmol/kg，皮下注射) 在 6-OHDA 损伤的大鼠中引发旋转行为(ED50=0.32 μmol/kg sc)。A-77636 (1-10 mg/kg) 以剂量依赖性方式减弱成瘾剂诱导的运动活动。A-77636 在大鼠 (ED50=12.3 μmol/kg s.c.) 和小鼠 (ED50=12.1 μmol/kg s.c.) 中产生前肢阵挛 。在用 MPTP 处理以诱导帕金森样状态的狨猴中，A-77636 (0.5、1.0 或 2.0 μmol/kg，口服)可增加运动活性并降低帕金森样症状的严重程度：该化合物在皮下或口服给药后均有活性。Animal Model:Rats with unilateral 6-OHDA (6-hydroxydopamine) lesions of the nigrostriatal pathway (six/group)
Dosage:0.32, 1.0, 3.2 μmol/kg
Administration:Subcutaneously
Result:Elicited prolonged (> 20 h) contralateral turning, which was blocked by SCH 23390, a D1 receptor antagonist, but not by haloperidol at doses selective for the dopamine D2 receptor.
Animal Model:Male Swiss Webster mice (18-25 g, five or six per cage)
Dosage:1, 3, 10 mg/kg
Administration:
Result:Attenuated addiction-induced locomotor activity in a dose-dependent manner. When administered alone, 1 and 3 mg/kg A-77636 produced little change in locomotor activity, whereas 10 mg/kg produced a significant and substantial decrease in locomotor activity.
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