阿醋美沙朵 | 17199-58-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 阿醋美沙朵
• 英文名称: L-α-acetylmethadol
• 英文别名: Alphacetylmethadol；[(3R,6R)-6-(dimethylamino)-4,4-diphenylheptan-3-yl] acetate
• CAS: 17199-58-5
• 化学式: C₂₃H₃₁NO₂
• 分子量: 353.505
• InChiKey: XBMIVRRWGCYBTQ-XMSQKQJNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  26
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  3

ADMET

代谢

醋酸阿尔法甲adol已知的人类代谢物包括norLAAM。

Alphacetylmethadol has known human metabolites that include norLAAM.

来源:NORMAN Suspect List Exchange

反应信息

• 作为产物：
  描述：

  乙酸酐 、 alkaline earth salt of/the/ methylsulfuric acid 在 吡啶 作用下， 生成 阿醋美沙朵
  参考文献：
  名称：

  与陨石有关的旋光化合物。

  摘要：

  DOI：

  10.1021/ja01170a025

文献信息

• ABUSE DETERRENT AND ANTI-DOSE DUMPING PHARMACEUTICAL SALTS USEFUL FOR THE TREATMENT OF ATTENTION DEFICIT/HYPERACTIVITY DISORDER
  申请人：King Clifford Riley

  公开号：US20120028960A1

  公开（公告）日：2012-02-02

  A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

  一种药物组合物，包括基本上由含有药用活性化合物的胺的药用可接受的有机酸加合盐组成的药物物质，其中含有药用活性化合物的胺被选择自光学异构体或单异构体利他林酸或苯乙胺衍生物的群体，并且该药物物质具有从无定形到多型的物理形式。
• SAFETY OF PSUEDOEPHEDRINE DRUG PRODUCTS
  申请人：King Clifford Riley

  公开号：US20140178480A1

  公开（公告）日：2014-06-26

  Drug substances comprising a amine containing pharmaceutically active compound, and at least one of an alditol acetal and an aromatic organic acid as an addition salt or an additive.

  含有胺基药用活性化合物的药物物质，以及至少一种醛糖醚和芳香有机酸中的一种作为附加盐或添加剂。
• Salts of physiologically active and psychoactive alkaloids and amines simultaneously exhibiting bioavailability and abuse resistance
  申请人：Bristol David William

  公开号：US20080293695A1

  公开（公告）日：2008-11-27

  Drug substances comprising a pharmaceutically acceptable organic acid addition salt 6f amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.

  包含药用可接受的有机酸盐的药物物质，其中含有药用活性化合物，用于治疗治疗性疾病管理，并在非治疗管理中使用时展现预防性特性。
• [EN] AN OPIOID FOR USE TO REDUCE AND/OR TREAT DRUG ADDICTION<br/>[FR] OPIOÏDE DESTINÉ À ÊTRE UTILISÉ POUR RÉDUIRE ET/OU TRAITER LA PHARMACODÉPENDANCE
  申请人：VERSI GROUP LLC

  公开号：WO2018204163A1

  公开（公告）日：2018-11-08

  The present invention relates to a method of treating drug addiction and reducing dependence or tolerance on a dependence-inducing opiate drug, wherein the method comprises administering to a subject a compound having the structure of formula (I): having the IUPAC name of (-)3-((S)-((2S,5R)-4-allyl-2,5-dimethyl-l-piperazinyl)(3-thienyl)methyl)phenol, or pharmaceutically acceptable esters or salts thereof, wherein the compound has activity on the mu, delta and kappa opioid receptors thereby providing added analgesia with an improved therapeutic index and reduced risk of respiratory depression.

  本发明涉及一种治疗药物成瘾、减少对诱导依赖的鸦片类药物的依赖或耐受性的方法，其中该方法包括向受试者施用具有以下公式（I）结构的化合物：(-)3-((S)-((2S,5R)-4-烯丙基-2,5-二甲基-1-哌嗪基)(3-噻吩基)甲基)苯酚的IUPAC名称，或其药学上可接受的酯或盐，化合物对mu、delta和kappa阿片受体具有活性，从而提供具有改善的治疗指数和减少呼吸抑制风险的附加镇痛作用。
• Abuse-deterrent pharmaceutical compositions of opiods and other drugs
  申请人：Collegium Pharmaceuticals, Inc.

  公开号：US20040052731A1

  公开（公告）日：2004-03-18

  An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

  已经开发了一种滥用抑制药物组合物，旨在降低药物的不当使用的可能性，特别是像阿片类药物这样的药物。在优选实施例中，药物被改性以增加其亲脂性。在优选实施例中，改性药物均匀分散在由缓慢溶解或不溶于水的材料组成的微粒中。在某些实施例中，含药微粒或药物颗粒被涂覆上一层或多层涂层，其中至少一层涂层是不溶于水且最好是有机溶剂不溶性的，但可被人类胃肠道中存在的酶降解。即使该组合物的物理完整性被破坏（例如通过切割或压碎）， resulting material仍然被放入水中、吸入或吞咽，该滥用抑制组合物也会延缓药物的释放。然而，当按照指示使用时，药物会缓慢地从组合物中释放出来，因为组合物会逐渐被酶降解、胆汁酸的表面活性作用和机械侵蚀逐渐破坏或溶解在胃肠道内。