Hydron;2-[6-(2-hydroxy-2-phenylethyl)-1-methylpiperidin-2-yl]-1-phenylethanone;chloride

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: Hydron;2-[6-(2-hydroxy-2-phenylethyl)-1-methylpiperidin-2-yl]-1-phenylethanone;chloride
• 化学式: C22H28ClNO2
• 分子量: 373.9
• InChiKey: MKMYPTLXLWOUSO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.66
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  40.5
• 氢给体数：
  2
• 氢受体数：
  3

ADMET

毒理性

• 人类毒性摘录

人类已经通过口腔容忍了8毫克的剂量，但有人报告出现恶心和上腹部疼痛。与尼古丁一样，中枢神经刺激之后会出现严重的抑郁，有时甚至因呼吸麻痹而死亡。/LOBELINE（及其盐类）/

HUMANS HAVE TOLERATED 8 MG BY MOUTH BUT SOME REPORTED NAUSEA & EPIGASTRIC PAIN. AS WITH NICOTINE, CENTRAL NERVOUS STIMULATION IS FOLLOWED BY SEVERE DEPRESSION & SOMETIMES DEATH IN RESPIRATORY PARALYSIS. /LOBELINE (& SALTS)/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 非人类毒性摘录

皮下剂量10毫克/千克常规导致狗呕吐，而在12毫克/千克时，一些动物经历了兴奋和抽搐。/洛贝林（及其盐类）/

SUBCUTANEOUS DOSES OF 10 MG/KG REGULARLY PRODUCED VOMITING IN DOGS & AT 12 MG/KG SOME ANIMALS EXPERIENCED EXCITEMENT & CONVULSIONS. /LOBELINE (& SALTS)/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 非人类毒性摘录

紫罗兰含有几种密切相关的生物碱，其中最重要的是山梗菜碱，它的作用类似于尼古丁和毒芹碱，首先刺激然后使自主神经节瘫痪。/紫罗兰/

THE LOBELIAS CONTAIN SEVERAL CLOSELY RELATED ALKALOIDS, THE MOST IMPORTANT BEING LOBELINE, WHICH RESEMBLES NICOTINE & CONIINE IN ITS ACTION, CAUSING FIRST STIMULATION THEN PARALYSIS OF THE AUTONOMIC GANGLIA. /LOBELIAS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 非人类毒性摘录

Lobelia berlandier 在墨西哥有毒性记录。在以0.5%体重的剂量对绵羊进行实验性喂食后，它引起了瞳孔散大、行动迟缓、食欲不振和腹泻，随后出现口腔溃疡、流涎和死亡。/Lobeline berlandier/

Lobelia berlandier has poisoned stock in Mexico. Fed experimentally to a sheep at a level of 0.5% body weight, it caused mydriasis, sluggishness, inappetence and diarrhea, followed by ulceration of the mouth, salivation, and death. /Lobeline berlandier/

来源:Hazardous Substances Data Bank (HSDB)

文献信息

• Use of sigma receptor ligands for the prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (IC/BPS)
  申请人：Laboratorios del Dr. Esteve S.A.

  公开号：EP2818166A1

  公开（公告）日：2014-12-31

  The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat pain associated to interstitial cystitis/bladder pain syndrome (IC/BPS).

  该发明涉及使用sigma配体，特别是配体（I）的sigma配体，以预防和/或治疗与间质性膀胱炎/膀胱疼痛综合症（IC/BPS）相关的疼痛。
• Medicated plasters
  申请人：NITTO DENKO CORPORATION

  公开号：EP0387751A2

  公开（公告）日：1990-09-19

  Medicated plasters composed of a flexible support and a pressure-sensitive adhesive layer laminated thereon, in which said pressure-sensitive adhesive layer has an exposed surface with pH of 7 or higher and contains one of the following three components: (i) a basic physiologically active agent and an acidic substance, (ii) a salt of a basic physiologically active agent and a basic substance, and (iii) a basic physiolosically active agent and a salt of a basic physiolosically active agent.

  药用膏药，由柔性支架和层压在其上的压敏胶层组成，其中所述压敏胶层的外露表面 pH 值为 7 或更高，并含有以下三种成分之一： (i) 碱性生理活性剂和酸性物质、 (ii) 碱性生理活性剂和碱性物质的盐，以及 (iii) 碱性生理活性剂和碱性生理活性剂的盐。
• Adhesive device for transdermal administration of an active agent
  申请人：NITTO DENKO CORPORATION

  公开号：EP0452837A2

  公开（公告）日：1991-10-23

  A medical adhesive comprising a plaster layer containing the following ingredients, characterized in that the ingredient ② is incorporated in a larger amount than the ingredient ⑤ and in an amount not less than 25% by weight relative to the total amount of the ingredients ①∼⑤, and the plaster layer is a W/O type : ① a medicinal ingredient, ② a hydrophobic polymer having a glass transition temperature (Tg) of -65°C to 35°C, ③ a percutaneous absorption-promoting agent, ④ water, and ⑤ a hydrophilic polymer which is soluble or capable of swelling in water; and a medical adhesive which comprises a porous base layer in the plaster layer or in contact with the plaster layer, which enable stable release of the medicinal ingredient, the percutaneous absorption-promoting agents and so on and sustaining of the pharmacological effects over a long period.

  一种医用粘合剂，由含有下列成分的石膏层组成，其特征在于，成分②的掺入量大于成分⑤，且相对于成分①∼⑤的总掺入量不低于 25%（重量百分比），石膏层为 W/O 型： 药物成分、 一种疏水性聚合物，其玻璃转化温度（Tg）为-65°C 至 35°C、 经皮吸收促进剂、 水，以及 可溶于水或能在水中溶胀的亲水性聚合物；以及 一种医用粘合剂，由石膏层中的多孔基底层或与石膏层接触的多孔基底层组成，可使药物成分、促进经皮吸收剂等稳定释放，并长期保持药理作用。
• CRYSTALLINE CONDITION DISLOCATING METHOD
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0665009A1

  公开（公告）日：1995-08-02

  An object of this invention is to provide a method of dislocating the crystalline condition of crystalline medicine simply, speedily and homogeneously, and, moreover, in large quantities at once. This invention is directed to a method using an extruder when crystalline medicine in a certain crystalline condition (△ is dislocated to another crystalline condition (○), i.e., when the dislocation of crystalline condition (△->○) is carried out.

  本发明的目的是提供一种简单、快速和均匀地将结晶药物的结晶状态变位的方法，而且是一次性大量变位。本发明针对的是一种使用挤压机将某种结晶状态（△）的结晶药物变位到另一种结晶状态（○）的方法，即结晶状态（△->○）变位的方法。
• PATCH
  申请人：HISAMITSU PHARMACEUTICAL CO. INC.

  公开号：EP1552822A1

  公开（公告）日：2005-07-13

  The present invention relates to a patch which is free from any migration of a drug into a substrate and has favorable anchoring properties between the substrate and a adhesive layer, in which the drug-containing adhesive layer firmly adheres onto the substrate and which gives no adhesive residue when applied to the skin and then peeled off. Namely, a patch comprising a substrate made of a polyester-based film and a drug-containing adhesive layer laminated thereon wherein the surface roughness of the polyester-based film surface in the side in contact with the adhesive layer is from 0.05 to 0.8 µmRa is provided.

  本发明涉及一种贴片，该贴片不含任何迁移到基底中的药物，并且在基底和粘合剂层之间具有良好的锚定特性，其中含药粘合剂层牢固地粘合在基底上，贴在皮肤上剥离时没有粘合剂残留。即，提供一种贴片，包括由聚酯薄膜制成的基底和层压在其上的含药粘合剂层，其中聚酯薄膜表面与粘合剂层接触面的表面粗糙度为 0.05 至 0.8 µmRa。

表征谱图