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  4. Org 9616 bromide

Org 9616 bromide 是一种非去极化神经肌肉阻滞剂，其结构与 Pancuroniam 类似。Org 9616 bromide 可诱导起效迅速、持续时间短的神经肌肉阻滞。

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Org 9616 bromide

Org 9616 bromide Chemical Structure

CAS No. : 119302-18-0

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Org 9616 bromide 相关抗体

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  • 生物活性

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生物活性

Org 9616 bromide is a non-depolarizing neuromuscular blocker with a structure similar to Pancuroniam. Org 9616 bromide induces rapid-onset, short-duration neuromuscular blockade[1].

药代动力学
(Parmacokinetics)
Species Dose Route T1/2 (Distribution) T1/2β V1 Vdss CL MRT
Cat[1] 1.2 mg/kg i.v. 2.5 min 25.9 min 149 mL/kg 346 mL/kg 28.2 mL/min/kg 11.1 min
体内研究
(In Vivo)

Org 9616 (1.2 mg/kg；静脉注射；推注) bromide 可在健康猫体内产生短效神经肌肉阻滞作用，1.2 mg/kg 静脉推注剂量下的作用时长为 14.6 分钟，其清除途径为生物转化和胆汁排泄[1]。
Org 9616 (1.2 mg/kg；静脉注射；推注) bromide 可使肾蒂结扎的猫产生短效神经肌肉阻滞，在 1.2 mg/kg 静脉推注剂量下作用时长为 15.4 分钟，且肾蒂结扎会缩短其恢复指数，同时延长消除半衰期和平均滞留时间[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: either sex, 2-4 kg[1]
Dosage: 1.2 mg/kg
Administration: i.v.; bolus
Result: Achieved onset time to maximum twitch depression of 0.7 minutes.
Reached duration of action (time to 25% twitch recovery) of 14.6 minutes.
Attained recovery index (25-75% twitch recovery) of 6.3 minutes.
Excreted 4.6% of the dose unchanged in urine, 20.4% unchanged in bile, and left 4.2% unchanged in the liver over 8 hours.
Excreted 1.4% of the dose as the 3-desacetyl metabolite in urine, 15.3% in bile, and left 9.8% in the liver over 8 hours.
Achieved total recovery of parent drug plus metabolite of 65% of the injected dose.\nAchieved onset time to maximum twitch depression of 0.5 minutes.
Reached duration of action (time to 25% twitch recovery) of 15.4 minutes.
Attained recovery index (25-75% twitch recovery) of 3.8 minutes, which was significantly shorter than in cats with intact renal pedicles (P < 0.05).
Showed prolonged mean elimination half-life and longer mean residence time compared to cats with intact renal pedicles.
Excreted 27.7% of the dose unchanged in bile, and left 3.6% unchanged in the liver over 8 hours.
Excreted 19.1% of the dose as the 3-desacetyl metabolite in bile, and left 14.5% in the liver over 8 hours.
Achieved total recovery of parent drug plus metabolite of 55% of the injected dose.
分子量

665.78

Formula

C36H61BrN2O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Org 9616 bromide 相关分类

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Keywords:

Org 9616119302-18-0Org9616Org-9616Drug DerivativeDrug derivativerenal pedicle ligationneuromuscular junction nicotinic acetylcholine receptorsuccinylcholinehepatic exclusionneuromuscular blockadeneuromuscular blocking agent3-desacetyl metabolitebiliary excretioncatsvecuroniumInhibitorinhibitorinhibit

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