(+/-)-trans-U-50488 methanesulfonate salt | 83913-06-8

• 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: (+/-)-trans-U-50488 methanesulfonate salt
• 英文别名: 2-(3,4-dichlorophenyl)-N-methyl-N-[(1R,2R)-2-pyrrolidin-1-ylcyclohexyl]acetamide;methanesulfonic acid
• CAS: 83913-06-8
• 化学式: C20H30Cl2N2O4S
• 分子量: 465.4
• InChiKey: OJPHNZCUXUUVKU-JAXOOIEVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.91
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.65
• 拓扑面积：
  86.3
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• PAIN THRESHOLD FALL INHIBITOR
  申请人：SANTEN PHARMACEUTICAL CO., LTD.

  公开号：EP1642590A1

  公开（公告）日：2006-04-05

  The invention aims to provide a drug having an activity on inhibiting a decrease in pain threshold. Since a κ-opioid receptor agonist effectively inhibits the decrease in pain threshold, it is useful as an inhibitor of pain threshold decrease.

  本发明旨在提供一种具有抑制痛阈降低活性的药物。由于κ-阿片受体激动剂能有效抑制痛阈的降低，因此它可以作为痛阈降低的抑制剂。
• Use of antagonists of PYY receptors for treating irritable bowel syndrome
  申请人：Cedars-Sinai Medical Center

  公开号：EP1875909A2

  公开（公告）日：2008-01-09

  The present invention concerns the use of antagonists of peptide YY receptors for treating irritable bowel syndrome (IBS) in a human subject. The antagonists may be used in conjunction with antagonists of serotonin receptors, calcitonin gene-related peptide or functional analogs thereof, adrenoceptors, or opioid receptors.

  本发明涉及使用肽 YY 受体拮抗剂治疗人类肠易激综合征（IBS）。拮抗剂可与血清素受体、降钙素基因相关肽或其功能类似物、肾上腺素受体或阿片受体的拮抗剂结合使用。
• Use of antagonists of PPY receptors for treating visceral pain or visceral hypersensitivity
  申请人：Cedars-Sinai Medical Center

  公开号：EP1891963A1

  公开（公告）日：2008-02-27

  The present invention relates to the use of a pharmaceutically acceptable composition comprising an active agent for oral or enteral delivery to a human subject for treating visceral pain or visceral hypersensitivity. The active agent may be an antagonist of peptide YY receptors which is used in an amount effective for reducing the sensation of esophageal, gastric, biliary, intestinal, colonic or rectal pain in the human subject.

  本发明涉及一种药学上可接受的组合物的用途，该组合物包含一种活性剂，用于口服或肠内给药给人类受试者，以治疗内脏疼痛或内脏过敏症。该活性剂可以是肽 YY 受体的拮抗剂，其用量可有效减轻人体的食管、胃、胆道、肠道、结肠或直肠疼痛的感觉。
• Use of PYY analogs and antagonists of PPY receptors for manipulating satiety
  申请人：Cedars-Sinai Medical Center

  公开号：EP1905446A1

  公开（公告）日：2008-04-02

  The present invention relates to uses of peptide YY, a peptide YY functional analog or an antagonist of receptors for peptide YY for manipulating satiety in mammals. Peptide YY or a peptide YY functional analog may be used for inducing satiety whereas antagonists of receptors for peptide YY may be used for suppressing satiety in mammals.

  本发明涉及肽YY、肽YY功能类似物或肽YY受体拮抗剂在操纵哺乳动物饱腹感方面的用途。肽 YY 或肽 YY 功能类似物可用于诱导饱腹感，而肽 YY 受体的拮抗剂可用于抑制哺乳动物的饱腹感。
• The treatment of small intestinal bacterial overgrowth (SIBO) and SIBO-related conditions
  申请人：Cedars-Sinai Medical Center

  公开号：EP2305213A2

  公开（公告）日：2011-04-06

  The present invention concerns pharmaceutically acceptable compositions, which may comprise a stabilizer of mast cell membranes in the lumenal wall of the small intestine, in an amount sufficient to inhibit a mast cell-mediated immune response in a human subject, for use as a medicament for treating small intestinal bacterial overgrowth (SIBO) or a SIBO-caused condition in a human subject in which the presence of SIBO has been detected.

  本发明涉及药学上可接受的组合物，该组合物可包含一种小肠腔壁肥大细胞膜稳定剂，其用量足以抑制人类受试者肥大细胞介导的免疫反应，可用作治疗小肠细菌过度生长（SIBO）或已检测到存在 SIBO 的人类受试者中 SIBO 引起的病症的药物。