Sugammadex sodium 是合成的 γ 环糊精衍生物,是一种新型的神经肌肉阻断逆转剂。
产品描述
Sugammadex, a synthetic derivative of γ-cyclodextrin, is a steroid-based neuromuscular blocker reversing agent.
体内活性
Injection of 100 microg/kg rocuronium resulted in a mean neuromuscular blockade of 93.0%, and profound blockade was achieved by injection of 500 microg/kg. After injection of the high rocuronium dose, the 90% recovery of the train-of-four ratio took 28 min after saline, 26 min after 1 mg/kg sugammadex, and 8 min after 2.5 mg/kg sugammadex. Signs of residual blockade or recurarization were not observed [1]. Treatment with 16 mg/kg and 100 mg/kg sugammadex had a neuroprotective effect in a transient global cerebral I/R rat model. However, 100 mg/kg sugammadex was more neuroprotective in rats [2].
动物实验
The animals were anesthetized with 80 mg/kg ketamine hydrochloride and 12 mg/kg xylazine administered intraperitoneally. After the rats were anesthetized, the bilateral common carotid arteries were exposed and carefully separated from the carotid sheath and the cervical sympathetic and vagal nerves through a ventral cervical incision. The bilateral common carotid arteries were occluded with nontraumatic aneurysm clips in ischemic rats but were not clamped in sham-operated rats. Complete interruption of the blood flow was confirmed by observing the central artery in the retina with an ophthalmoscope. The body temperature of the rats was maintained at 37.0 ± 0.5°C during this procedure. In this model, 10 minutes of ischemia and 24 hours of reperfusion were induced. After the ischemic period, the rats were treated with sugammadex 16 mg/kg (S 16 group) and sugammadex 100 mg/kg (S 100 group) (intravenous and total volume 1 mL) in the 5th minute of reperfusion. Sugammadex was diluted with normal saline (0.9% NaCl). The same surgical procedure was performed in the I/R group, but the rats were not treated with sugammadex. The neck incision was closed with sutures (3.0 silk), and the animals were allowed to awaken. After 24 hours, the neurological condition of the rats was assessed with a scoring system [2].
Cas No.
343306-79-6
分子式
C72H104Na8O48S8
分子量
2177.97
别名
Sugammadex (sodium);舒更葡糖钠;Org25969;Sugammadex sodium
储存和溶解度
H2O:34 mg/mL (15.61 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years