溴胍喹定 | 154-73-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 四氢异喹啉
• 中文名称: 溴胍喹定
• 中文别名: 胍尼索喹
• 英文名称: 7-bromo-3,4-dihydro-1H-isoquinoline-2-carboximidic acid amide
• 英文别名: Guanisoquine；7-bromo-3,4-dihydro-1H-isoquinoline-2-carboximidamide
• CAS: 154-73-4
• 化学式: C₁₀H₁₂BrN₃
• 分子量: 254.129
• InChiKey: ICLLENNEPRZLAP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  53.1
• 氢给体数：
  2
• 氢受体数：
  1

安全信息

• 海关编码：
  2933499090

文献信息

• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Process for producing amidine sulfonic acid intermediates for guanidines
  申请人：McNeilab, Inc.

  公开号：EP0248586A2

  公开（公告）日：1987-12-09

  An efficient synthesis of quanidines, e.g. of the formula (III), by oxidizing a thiourea, e.g. of the following formula (II): with H₂O₂ and a molybdenum catalyst to yield an aminoiminomethane sulfonic acid which can then be reacted with an amine followed by optional transamination steps.

  一种通过氧化硫脲（例如下式(II)）高效合成胍类（例如式(III)）的方法： 与 H₂O₂和钼催化剂氧化，生成氨基亚氨基甲烷磺酸，然后与胺反应，再进行任选的转氨基步骤。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• Serotonin transporter gene and treatment of opioid-related disorders
  申请人：University of Virginia Patent Foundation

  公开号：US10995374B2

  公开（公告）日：2021-05-04

  The gene responsible for encoding SERT has a functional polymorphism at the 5′-regulatory promoter region, which results in two forms, long (L) and short (S). The LL-genotype is hypothesized to play a key role in the early onset of alcohol use. The present invention discloses the differences in treatment and diagnosis based on the L or short genotypes as well as on a single nucleotide polymorphism of the SERT gene, the 3′ UTR SNP rs1042173. The present invention demonstrates the efficacy of using the drug ondansetron and similar drugs for treatment based on variations in the polymorphisms of the SERT gene as well as methods for diagnosing susceptibility to abuse of alcohol and other addiction-related diseases and disorders.

  负责编码 SERT 的基因在 5′调控启动子区域存在功能性多态性，可分为长型（L）和短型（S）两种。据推测，LL 基因型在早期饮酒中起着关键作用。本发明公开了基于 L 或短基因型以及 SERT 基因的单核苷酸多态性（3′UTR SNP rs1042173）的治疗和诊断差异。本发明展示了根据 SERT 基因多态性的变异使用昂丹司琼和类似药物进行治疗的疗效，以及诊断酗酒易感性和其他成瘾相关疾病和障碍的方法。
• EP0573581A4
  申请人：——

  公开号：EP0573581A4

  公开（公告）日：1994-06-29