6-Propyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-2,10,11-triol | 586391-22-2

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 阿朴菲
• 英文名称: 6-Propyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-2,10,11-triol
• CAS: 586391-22-2
• 化学式: C₁₉H₂₁NO₃
• 分子量: 311.4
• InChiKey: HLRBSTGXOFUEHW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  63.9
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• N-substituted aporphines, a method of inducing emesis and a method of controlling psychosis utilising the same
  申请人：NORTHEASTERN UNIVERSITY

  公开号：EP0040074A1

  公开（公告）日：1981-11-18

  N-substituted aporphines of the formula wherein R, is lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, lower alkenyl, substituted lower alkenyl, lower alkynyl, substituted lower alkynyl, phenyl lower alkyl, phenyl lower alkenyl and phenyl lower alkynyl, R2 is hydrogen or wherein R3 is lower alkyl and R4 is hydrogen or R20 and the acid addition salts thereof with the proviso that when R4 is hydrogen R1 is 2-chloroethyl. Representative compounds of this invention are potent emetics and dopamine antagonists.

  式中的 N-取代卟吩 其中 R，是低级烷基、取代的低级烷基、环烷基、取代的环烷基、低级烯基、取代的低级烯基、低级炔基、取代的低级炔基、苯基低级烷基、苯基低级烯基和苯基低级炔基，R2 是氢或 其中 R3 为低级烷基，R4 为氢或 R20 及其酸加成盐，但当 R4 为氢时，R1 为 2-氯乙基。本发明的代表性化合物是强效的催吐剂和多巴胺拮抗剂。
• Polyglutamine repeat sequences
  申请人：——

  公开号：US20030162231A1

  公开（公告）日：2003-08-28

  Several neurodegenerative diseases result from the aggregation of polyglutamine repeat proteins into insoluble neuronal intranuclear inclusions. The invention provides methods with which to study the processes of these diseases, including methods for solubilizing polypeptides containing a polyglutamine repeat sequence, for storing these polyglutamine polypeptides and inhibit their spontaneous aggregation, for making the aggregates of polyglutamine polypeptides, for assaying the extension of existing polyglutamine aggregates, for determining the ability of a chemical compound to inhibit aggregation, and for inhibiting aggregation of polyglutamine polypeptides. The invention further provides materials with which to study these diseases including a synthetic aggregate that have a capability to recruit additional monomeric polyglutamine polypeptides and chemical compounds that inhibit the formation and/or extension of polyglutamine aggregates.

  一些神经退行性疾病是由多谷氨酰胺重复蛋白聚集成不溶性神经元核内包涵体引起的。本发明提供了研究这些疾病过程的方法，包括溶解含有多谷氨酰胺重复序列的多肽的方法、储存这些多谷氨酰胺多肽并抑制其自发聚集的方法、制造多谷氨酰胺多肽聚集体的方法、检测现有多谷氨酰胺聚集体扩展的方法、确定化合物抑制聚集能力的方法以及抑制多谷氨酰胺多肽聚集的方法。本发明进一步提供了用于研究这些疾病的材料，包括具有招募额外多聚谷氨酰胺多肽单体能力的合成聚集体和抑制多聚谷氨酰胺聚集体形成和/或延伸的化合物。
• DOPAMINE AND AGONISTS AND ANTAGONISTS THEREOF FOR MODULATION OF SUPPRESSIVE ACTIVITY OF CD4+CD25+ REGULATORY T CELLS
  申请人：YEDA RESEARCH AND DEVELOPMENT CO. LTD.

  公开号：EP1626703A2

  公开（公告）日：2006-02-22
• Dopamine and agonists and antagonists thereof for modulation of suppressive activity of CD4+CD25+ regulatory T cells
  申请人：Eisenbach-Schwartz Michal

  公开号：US20100168085A1

  公开（公告）日：2010-07-01

  Compositions and methods for modulation of the suppressive activity of CD4+CD25+regulatory T cells (Treg) on CD4+CD25− effector T cells (Teff) are provided. An agent selected from: (i) dopamine; (ii) a dopamine precursor; (iii) a D1-R agonist; (iv) a D2-R antagonist; (v) a combination of (i) and (ii); or (vi) a combination of (i), (ii) or (iii) with (iv), down-regulates the suppressive activity of Treg and is useful for treatment of cancer. An agent selected from (i) a dopamine D2-R agonist, (ii) a dopamine D1-R antagonist, and (iii) a combination of (i) and (ii), up-regulates the suppressive activity of Treg and is useful for treatment of an autoimmune disease or for controlling graft rejection in tissue/organ transplantation.
• DNA CYTOSINE DEAMINASE INHIBITORS
  申请人：Harris Reuben S.

  公开号：US20110218158A1

  公开（公告）日：2011-09-08

  Cytosine deaminase inhibitors and methods for identifying inhibitors of the anti-retroviral activity of APOBEC3G are described.