N,N-dimethyl-2-oxo-N-(2-oxo-2-(phenylamino)ethyl)-2-(phenylamino)ethane-1-aminium | 15272-69-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N,N-dimethyl-2-oxo-N-(2-oxo-2-(phenylamino)ethyl)-2-(phenylamino)ethane-1-aminium
• 英文别名: N,N-dimethyl-2-oxo-N-(2-oxo-2-(phenylamino)ethyl)-2-(phenylamino)ethan-1-aminium；N,N-bis(phenylaminoformylmethyl)dimethylammonium；N,N-Bis-(phenylcarbamoylmethyl)dimethylammonium；carcainium；bis(2-anilino-2-oxoethyl)-dimethylazanium
• CAS: 15272-69-2
• 化学式: C₁₈H₂₂N₃O₂
• 分子量: 312.392
• InChiKey: MPOXTHSNJVUPKR-UHFFFAOYSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  58.2
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• [EN] CARCAINIUM SALTS<br/>[FR] SELS DE CARCAÏNIUM
  申请人：VERONA PHARMA PLC

  公开号：WO2014037727A1

  公开（公告）日：2014-03-13

  A pharmaceutically acceptable addition salt of (i) carcainium, and (ii) oxalic acid, fumaric acid, maleic acid orhydrobromic acid.

  (i) 草果碱和(ii) 草酸、富马酸、马来酸或溴酸的药用可接受的加盐物。
• TREATING COUGH AND TUSSIVE ATTACKS
  申请人：Walker Michael J.A.

  公开号：US20140242174A1

  公开（公告）日：2014-08-28

  The invention is directed towards carcainium in the form of a salt having an anion An − , wherein An − is an anion of pharmaceutically acceptable acid for use in the treatment and/or suppression of cough, tussive attacks or tussive episodes in a patient.

  本发明涉及一种以盐的形式存在的Carcainium，其阴离子为An−，其中An−是一种药学上可接受的酸的阴离子，用于治疗和/或抑制患者的咳嗽、咳嗽发作或咳嗽症状。
• SENSORY-SPECIFIC LOCAL ANESTHESIA AND PROLONGED DURATION LOCAL ANESTHESIA
  申请人：Kohane Daniel S.

  公开号：US20110086922A1

  公开（公告）日：2011-04-14

  Combinations of charged local anesthetics with chemical permeation enhancers have been developed to give long duration block which is selective for sensory block over motor block. The duration of block is greatly prolonged by combining the local anesthetic with a permeation enhancer. The selectivity of sensory over motor block is provided by selecting the concentration of the local anesthetic and the permeation enhancer to provide selective permeability of the sensory and motor neurons to the enhancer.
• CHEMICAL PERMEATION ENHANCERS ENHANCE NERVE BLOCKADE BY TOXINS
  申请人：Kohane Daniel S.

  公开号：US20110237611A1

  公开（公告）日：2011-09-29

  Chemical permeation enhancers (CPEs) improve access of local anesthetics to the nerve, thereby improving their performance. Surfactants, representing three CPE sub-groups: anionic, cationic, and nonionic surfactants, were co-injected with tetrodotoxin (TTX) or bupivacaine at the sciatic nerve of Sprague-Dawley rats. All enhancers produced marked concentration-dependent improvements in the frequency and duration of block with TTX but not bupivacaine. An in vitro toxicity assay showed a wide range of CPE myotoxicity, but in vivo histological assessment showed no signs of muscle or nerve damage at concentrations of CPEs that produced a half-maximal increase in the duration of block of TTX. There was no systematic relationship between the enhancers' charge or hydrophobicity and their enhancement of block duration or potency. Thus, CPEs can provide marked prolongation of nerve blockade from TTX, without apparent local tissue toxicity, and therefore enhance the clinical applicability of TTX for prolonged-duration local anesthesia.
• Chemical Permeation Enhancers Enhance Nerve Blockade by Toxins
  申请人：Massachusetts Institute of Technology

  公开号：US20140080841A1

  公开（公告）日：2014-03-20

  Chemical permeation enhancers (CPEs) improve access of local anesthetics to the nerve, thereby improving their performance. Surfactants, representing three CPE sub-groups: anionic, cationic, and nonionic surfactants, were co-injected with tetrodotoxin (TTX) or bupivacaine at the sciatic nerve of Sprague-Dawley rats. All enhancers produced marked concentration-dependent improvements in the frequency and duration of block with TTX but not bupivacaine. An in vitro toxicity assay showed a wide range of CPE myotoxicity, but in vivo histological assessment showed no signs of muscle or nerve damage at concentrations of CPEs that produced a half-maximal increase in the duration of block of TTX. There was no systematic relationship between the enhancers' charge or hydrophobicity and their enhancement of block duration or potency. Thus, CPEs can provide marked prolongation of nerve blockade from TTX, without apparent local tissue toxicity, and therefore enhance the clinical applicability of TTX for prolonged-duration local anesthesia.