Sulamserod | 219757-90-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: Sulamserod
• 英文别名: N-[2-[4-[3-(5-amino-6-chloro-2,3-dihydro-1,4-benzodioxin-8-yl)-3-oxopropyl]piperidin-1-yl]ethyl]methanesulfonamide
• CAS: 219757-90-1
• 化学式: C₁₉H₂₈ClN₃O₅S
• 分子量: 446.0
• InChiKey: NBUGBCTWXCXBQD-UHFFFAOYSA-N

物化性质

• 沸点：
  647.8±65.0 °C(Predicted)
• 密度：
  1.319±0.06 g/cm3(Predicted)
• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  29
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.63
• 拓扑面积：
  119
• 氢给体数：
  2
• 氢受体数：
  8

制备方法与用途

生物活性 Sulamserod 是一种 5-HT4 受体拮抗剂，具有抗心律失常的功效。

靶点

• 5-HT₄ 受体

体内研究 Sulamserod (30 mg/kg) 在猪身上表现出以下效果：延长平均ERP（11,568 毫秒 vs 14,667 毫秒，P<0.01）和波长（8.36±0.9 厘米 vs 9.96±0.8 厘米，P<0.01），减少ERP离散度（1,565 毫秒 vs 861 毫秒，P<0.01），并轻微减缓传导速度（72.64 厘米/秒 vs 67.65 厘米/秒，P<0.01）。Sulamserod 对室性心律失常无明显影响。在8只动物中终止了6例房扑，在9只动物中终止了8例房颤，并防止所有动物出现持续性心动过速的再次发作。

文献信息

• The use of 5ht4 receptor antagonists in the prophylaxis or treatment of certain cardiovascular conditions
  申请人：Bonhomme Marguerite Jeanne Mireille

  公开号：US20050032866A1

  公开（公告）日：2005-02-10

  The invention relates to the use of a 5-HT 4 receptor antagonist in the manufacture of a medicament for the prophylaxis or treatment of atrial remodelling in a mammal. Preferably, the antagonist is N-[(1- n butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide (SB 207266) or a pharmaceutically acceptable salt thereof. The invention also relates to the use of SB 207266 or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for the treatment or prophylaxis of atrial fibrillation in a mammal by administering to the mammal a daily oral or parenteral dosage regimen of about 0.2 mg to 1.0 mg of the SB 207266 or salt thereof per kg of total body weight (measured as the free base). The invention also relates to the use of SB 207266 or a pharmaceutically acceptable salt thereof in the prophylaxis or treatment of atrial arrhythmia in a mammal by administration of the SB 207266 or salt thereof on the first day at a loading dose of about 1.2 to about 2.0 times the daily maintainance dose, followed by administration of the SB 207266 or salt at the daily maintainance dose on subsequent days.

  本发明涉及使用 5-HT 4 受体拮抗剂用于制造预防或治疗哺乳动物心房重塑的药物。优选地，拮抗剂是 N-[（1- n 丁基-4-哌啶基）甲基]-3,4-二氢-2H-[1,3]恶嗪并[3,2-a]吲哚-10-甲酰胺（SB 207266）或其药学上可接受的盐。本发明还涉及 SB 207266 或其药学上可接受的盐在制造用于治疗或预防哺乳动物心房颤动的药物中的用途，方法是向哺乳动物施用每日口服或肠外剂量方案，每公斤总重量（以游离碱计）约 0.2 毫克至 1.0 毫克 SB 207266 或其盐。本发明还涉及SB 207266或其药学上可接受的盐在预防或治疗哺乳动物房性心律失常中的用途，方法是第一天以约1.2至约2.0倍每日维持剂量的负荷剂量给药SB 207266或其盐，随后几天以每日维持剂量给药SB 207266或其盐。
• USE OF 5HT4 RECEPTOR ANTAGONISTS IN THE MANUFACTURE OF A MEDICAMENT FOR THE PROPHYLAXIS OR TREATMENT OF ATRIAL FIBRILLATION
  申请人：Laboratoire Glaxosmithkline S.A.S.

  公开号：EP1311295A2

  公开（公告）日：2003-05-21
• COMPOSITION PHARMACEUTIQUE POUR LA PREPARATION D'UN MEDICAMENT DESTINE A TRAITER ET/OU A PREVENIR UNE PATHOLOGIE LIEE A UNE CONDUITE OBSESSIONNELLE OU L'OBESITE
  申请人：CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)

  公开号：EP1556489B1

  公开（公告）日：2011-01-26
• USE OF 5HT4 RECEPTOR ANTAGONISTS IN THE PROPHYLAXIS OR TREATMENT OF CERTAIN CARDIOVASCULAR CONDITIONS
  申请人：Bonhomme Marguerite Jeanne Mireille

  公开号：US20070015769A1

  公开（公告）日：2007-01-18

  The invention relates to the use of a 5-HT 4 receptor antagonist in the manufacture of a medicament for the prophylaxis or treatment of atrial remodelling in a mammal. Preferably, the antagonist is N-[(1- n butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide (SB 207266) or a pharmaceutically acceptable salt thereof. The invention also relates to the use of SB 207266 or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for the treatment or prophylaxis of atrial fibrillation in a mammal by administering to the mammal a daily oral or parenteral dosage regimen of about 0.2 mg to 1.0 mg of the SB 207266 or salt thereof per kg of total body weight (measured as the free base). The invention also relates to the use of SB 207266 or a pharmaceutically acceptable salt thereof in the prophylaxis or treatment of atrial arrhythmia in a mammal by administration of the SB 207266 or salt thereof on the first day at a loading dose of about 1.2 to about 2.0 times the daily maintainance dose, followed by administration of the SB 207266 or salt at the daily maintainance dose on subsequent days.
• PHARMACEUTICAL COMPOSITION FOR TREATING AND/OR PREVENTING A PATHOLOGY ASSOCIATED WITH AN OBSESSIONAL BEHAVIOR OR WITH OBESITY
  申请人：Compan Valerie

  公开号：US20090124592A1

  公开（公告）日：2009-05-14

  This invention relates to the use of a ligand of the 5-HT 4 receptor or of a pharmaceutically acceptable salt of this ligand and to a nucleic acid coding for a 5-HT 4 receptor or of a functionally equivalent receptor for a drug for treating and/or preventing a pathology associated with an obsessional behavior such as anorexia, bulimia and the addiction to drugs of abuse or obesity. The invention also relates to a method for identifying a compound that is biologically active in the treatment and/or the prevention of a pathology associated with an obsessional conduct or obesity including: a) placing the 5-HT 4 receptor or a functionally equivalent receptor in contact with this biologically active compound, and b) the determination of whether this biologically active compound is capable of modulating the basal activity of the 5-HT 4 receptor or of a functionally equivalent receptor.