Hexamethonium Dibromide是一种神经中枢中选择性的神经元烟碱型AChR选择性拮抗剂。
| Target | Value |
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Dopamine subtype 2 receptor
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AChR
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Hexamethonium Bromide能有效抵抗Ach和卡巴胆碱(CCh)对大鼠肩胛舌骨肌终板振幅的响应，EC50分别为300 μM和100 μM。0.6 μM 筒箭毒碱存在下，Hexamethonium Bromide (50-200 μM)使神经诱发的终板电流(e.p.cs)的振幅增加。在大鼠肌肉匀浆中，Hexamethonium Bromide也是乙酰胆碱酯酶活性的弱抑制剂，EC50为1.5 mM。在大鼠一侧膈肌中，Hexamethonium Bromide (200 μM)降低终板电流(e.p.cs) (降低~25%)和微终板电流(m.e.p.cs) (降低~20%)衰变的时间常数。在低频刺激(0.5-2 Hz)下，Hexamethonium Bromide (200 μM)增加30-40% e.p.c.量子含量。
Hexamethonium Bromide (0.2-25 mg/kg; i.v.) significantly reduces the renal sympathetic nerve activity (RSNA), mean arterial pressure (MAP) and heart rate (HR) in the Wistar rats and the spontaneously hypertensive rats (SHRs).
Hexamethonium Bromide (0.2-1.0 mg/kg; i.v.) treatments show no significant differences in the RSNA, MAP or HR between Wistar rats and SHRs.
Hexamethonium Bromide (5.0-25 mg/kg; i.v.) results in a greater reduction in the RSNA and MAP in SHRs compared with Wistar rats.
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Animal Model:
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Male normotensive Wistar rats (280-320 g), SHRs
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Dosage:
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0.2 mg/kg, 1.0 mg/kg, 5.0 mg/kg, 25 mg/kg
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Administration:
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Intravenous injection
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Result:
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Significantly reduced the RSNA, MAP and HR in the Wistar rats and the SHRs.
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