Rapacuronium | 465499-11-0

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: Rapacuronium
• 英文别名: [(2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-3-acetyloxy-10,13-dimethyl-2-piperidin-1-yl-16-(1-prop-2-enylpiperidin-1-ium-1-yl)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl] propanoate
• CAS: 465499-11-0
• 化学式: C37H61N2O4+
• 分子量: 597.9
• InChiKey: HTIKWNNIPGXLGM-YLINKJIISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.6
• 重原子数：
  43
• 可旋转键数：
  9
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  55.8
• 氢给体数：
  0
• 氢受体数：
  5

ADMET

代谢

经水解转化为活性代谢物（细胞色素P450系统未参与）。

Hydrolyzed to active metabolites (Cytochrome P450 system is not involved).

来源:DrugBank

毒理性

• 蛋白质结合

变化。通过平衡透析法研究了瑞帕库隆（rapacuronium）在人血浆中的血浆蛋白结合情况。蛋白结合率在50%到88%之间变化，这至少部分是由于瑞帕库隆溴化物水解为其3-羟基代谢物所致。瑞帕库隆结合的特定血浆蛋白尚不清楚。未确定3-羟基代谢物的血浆蛋白结合情况。

Variable. Plasma protein binding of rapacuronium was studied in vitro for human plasma by equilibrium dialysis. The protein binding was variable and ranged between 50% and 88%, which was at least partly due to hydrolysis of rapacuronium bromide to its 3-hydroxy metabolite. The specific plasma protein to which rapacuronium binds is unknown. Plasma protein binding of the 3-hydroxy metabolite was not determined.

来源:DrugBank

文献信息

• STABILIZED AQUEOUS COMPOSITIONS OF NEUROMUSCULAR BLOCKING AGENTS
  申请人：B. Braun Melsungen AG

  公开号：EP2900216B1

  公开（公告）日：2017-04-26
• Stabilized Aqueous Compositions of Neuromuscular Blocking Agents
  申请人：B. Braun Melsungen AG

  公开号：US20150216979A1

  公开（公告）日：2015-08-06

  The present invention relates to an aqueous composition comprising: (i) a quaternary ammonium neuromuscular blocking agent; and (ii) an excipient selected from a polyhydroxy acid of the following formula: HO—CH 2 —[CH(OH)] n —COOH, wherein n is an integer from 1 to 8, an intramolecular lactone of said polyhydroxy acid or a mixture thereof. Furthermore the present invention relates to a liquid pharmaceutical composition comprising or consisting of said aqueous composition and a method for producing said aqueous composition comprising the steps of: a) providing a quaternary ammonium neuromuscular blocking agent wherein said quaternary ammonium neuromuscular blocking agent is optionally freeze-dried, b) providing an excipient selected from a polyhydroxy acid of the following formula: HO—CH 2 —[CH(OH)] n —COOH, wherein n is an integer from 1 to 8, an intramolecular lactone of said polyhydroxy acid or a mixture thereof, wherein said excipient is optionally freeze-dried, c) mixing the quaternary ammonium neuromuscular blocking agent of step a) and the excipient of step b) in water to give an aqueous composition. In addition, the present invention relates to the use of a polyhydroxy carboxylic acid of the following formula: HO—CH 2 —[CH(OH)] n —COOH, wherein n is an integer from 1 to 8, an intramolecular lactone of said polyhydroxy acid or a mixture thereof for stabilizing an aqueous composition comprising a quaternary ammonium neuromuscular blocking agent. The present invention also refers to a container containing the aqueous composition or the liquid pharmaceutical composition of the present invention. It furthermore relates to a kit comprising said compositions. Preferred embodiments are apparent from the dependent claims.
• ACYCLIC CUCURBIT[N]URIL TYPE MOLECULAR CONTAINERS TO TREAT INTOXICATION AND DECREASE RELAPSE RATE IN SUBSTANCE ABUSE DISORDERS
  申请人：UNIVERSITY OF MARYLAND, COLLEGE PARK

  公开号：US20170246180A1

  公开（公告）日：2017-08-31

  Provided are methods for reversing the effects of drugs of abuse. The method involves administering acyclic CB[n]-type compounds to a mammal in need of the reversal of the effects from a drug of abuse.
• US9469648B2
  申请人：——

  公开号：US9469648B2

  公开（公告）日：2016-10-18
• US9956229B2
  申请人：——

  公开号：US9956229B2

  公开（公告）日：2018-05-01