乙磺酸去痛定 | 42476-22-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 乙磺酸去痛定
• 英文名称: Piminodine esylate
• 英文别名: ethanesulfonic acid;ethyl 1-(3-anilinopropyl)-4-phenylpiperidine-4-carboxylate
• CAS: 42476-22-2；7081-52-9
• 化学式: C25H36N2O5S
• 分子量: 476.6
• InChiKey: PRERKVDQJAYTGE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.98
• 重原子数：
  33
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  104
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Neutral antagonists and use thereof in treating drug abuse
  申请人：——

  公开号：US20010049375A1

  公开（公告）日：2001-12-06

  The invention relates to the use of naltrexone and naloxone analogs, which are neutral antagonists at the &mgr; opioid receptor, for the treatment of drug dependency in a drug-dependent individual. Surprisingly, it has been found that administration of a therapeutically effect amount of the naloxone or naltrexone analogs described herein for the treatment of a drug dependency, can result in reduction of undesirable side effects resulting from current treatments using naloxone and naltrexone. For example, the treatment described herein can result in a reduction in the withdrawal symptoms and aversion encountered in the use of naloxone and naltrexone in the treatment of drug dependency. In addition, the naltrexone and naloxone analogs of the invention can be used for the treatment of pain in an individual in need thereof by modulating opoid pain treatment using neutral antagonists, for example, reversing respiratory depression withough causing other adverse effects. In addition, during chronic use of opioid drugs for pain therapy, neutral antagonists can be used to diminish constipation peripherally without effecting the central analgesic effects.

  本发明涉及纳曲酮和纳洛酮类似物的用途，它们是&mgr;阿片受体的中性拮抗剂，用于治疗药物依赖者的药物依赖性。令人惊奇的是，研究发现，在治疗药物依赖性时，施用一定治疗效果量的本文所述纳洛酮或纳曲酮类似物，可以减少目前使用纳洛酮和纳曲酮治疗所产生的不良副作用。例如，本文所述的治疗方法可以减少在使用纳洛酮和纳曲酮治疗药物依赖性时遇到的戒断症状和厌恶感。此外，本发明的纳曲酮和纳洛酮类似物可通过使用中性拮抗剂调节阿片类疼痛治疗，例如逆转呼吸抑制而不引起其他不良反应，从而用于治疗有需要的人的疼痛。此外，在长期使用阿片类药物治疗疼痛期间，中性拮抗剂可用于减轻外周性便秘，而不会影响中枢镇痛效果。
• Method and composition for reducing the danger and preventing the abuse of controlled release pharmaceutical formulations
  申请人：——

  公开号：US20030049317A1

  公开（公告）日：2003-03-13

  The present invention relates to a method and composition for reducing the danger and preventing the abuse of orally administered, controlled release, pharmaceutical formulations. These formulations are useful to prevent the abuse of or accidental overdose of such formulations which can be overdosed or abused by chewing or crushing the formulation prior to ingestion. The formulations comprise a therapeutic, pharmaceutical composition and an antagonist to the pharmaceutical composition which is only bioavailable upon chewing or crushing of the antagonist prior to oral administration of the pharmaceutical formulation.

  本发明涉及一种方法和组合物，用于降低口服控释药物制剂的危险性并防止其滥用。这些制剂有助于防止此类制剂的滥用或意外过量，因为在摄入前咀嚼或压碎制剂可导致过量或滥用。这些制剂包括一种治疗性药物组合物和一种药物组合物的拮抗剂，只有在口服该药物制剂之前咀嚼或碾碎拮抗剂，才能获得这种拮抗剂。
• NEUTRAL ANTAGONISTS AND USE THEREOF IN TREATING DRUG ABUSE
  申请人：Sadee, Wolfgang

  公开号：EP1263438B1

  公开（公告）日：2006-05-17
• NOVEL COMPOSITIONS AND METHODS
  申请人：Generics (UK) Limited

  公开号：EP2056875A1

  公开（公告）日：2009-05-13
• COMBINATION ANALGESIC EMPLOYING OPIOID AND NEUTRAL ANTAGONIST
  申请人：Aiko Biotechnology

  公开号：EP2214672B1

  公开（公告）日：2012-10-17