Pancuronium bromide是一种双季基类固醇,是一种神经肌肉松弛剂。它通过与乙酰胆碱竞争nACh受体上的结合位点来抑制神经肌肉传递。它还可抑制心脏毒蕈碱受体并具有拟交感神经作用。
产品描述
Pancuronium dibromide, a competitive AChR antagonist (IC50 = 5.5 nM), acts as a skeletal muscle relaxant. Pancuronium dibromide blocking neuromuscular transmission is achieved by competing with acetylcholine for receptor sites on the motor end-plate.
体外活性
Pancuronium?results in open?channel?block?of embryonic-type?nicotinic?acetylcholine receptor channels after coapplication of blocker and acetylcholine, characterized by decrease of the time constant of current decay. Pancuronium also results in?competitive?block?of embryonic-type?nicotinic acetylcholine receptor channels. [1] Pancuronium?increases heart rate,?vecuronium?and?rocuronium?produces positive inotropic?effects, and?vecuronium shortens refractoriness in isolated rat atria.? [2] Pancuronium (0.5 mM) induces a complete?fade?of the?tetanic contraction while leaving the twitch unaffected in the extensor digitorum longus muscle of the rat.?Pancuronium?decreases the amplitude and increases the?tetanic?rundown of trains of endplate potentials (e.p.ps) evoked in the frequency of 50 Hz in the extensor digitorum longus muscle of the rat.[3]
体内活性
Pancuronium?decreases tidal volume (VT) and minute ventilation (VE) in high dose?dogs by 82%. Pancuronium?decreases tidal volume (VT) and minute ventilation (VE) in low dose?dogs by 40% and 55%. [4] Pancuronium limits?cerebral?hyperemia during prolonged?seizures?by attenuating increases in?blood?pressure as a result of elimination of skeletal muscle activity in newborn pigs. [5] Pancuronium?results in a significant difference with control is observed at gallamine concentrations ranging from 0.032-0.32 mM ?in?tracheal?smooth muscle?strips from?guinea-pigs.[6]
Cas No.
15500-66-0
分子式
C35H60Br2N2O4
分子量
732.683
别名
Pancuronium bromide;Pavulon;泮库溴铵;Pancuronium dibromide
储存和溶解度
DMSO:136.5 mM
H2O:136.49mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years