Hexamethonium Bromide是神经节中神经元型烟碱型 AChR 的特异性拮抗剂。在自发性高血压动物模型中,它能降低其交感神经活动和血压。
产品描述
Hexamethonium Bromide, a specific antagonist of neuronal-type nicotinic AChR in ganglia, is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier.
体外活性
Hexamethonium Bromide is effective against Ach and carbachol (CCh) on the amplitude of endplate responses of rat omohyoid muscle with EC50 of 300 μM and 100 μM, respectively. Hexamethonium Bromide (50-200 μM) causes an increase in the amplitude of nerve-evoked endplate currents (e.p.cs) recorded in the presence of 0.6 μM tubocurarine. Hexamethonium Bromide is also a weak inhibitor of acetylcholinesterase activity in rat muscle homogenates with EC50 of 1.5 mM. [1] Hexamethonium Bromide (200 μM) decreases the time constant of decay of both endplate currents (e.p.cs) (by ~25%) and miniature endplate currents (m.e.p.cs) (by ~20%) in the rat hemi-diaphragm muscle. At low frequencies of stimulation (0.5-2 Hz), Hexamethonium Bromide (200 μM) increases e.p.c. quantal content by 30-40%. [2]
Cas No.
55-97-0
分子式
C12H30Br2N2
分子量
362.194
别名
Hexamethonium Dibromide;Gangliostat;Simpatoblock;溴化六甲铵;六甲溴铵
储存和溶解度
DMSO:18.1 mg/mL (50 mM)
H2O:36.2 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years