2,10,11-三羟基-N-n-丙基去甲阿朴啡

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 阿朴菲
• 中文名称: 2,10,11-三羟基-N-n-丙基去甲阿朴啡
• 英文名称: hydron;6-propyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-2,10,11-triol;bromide
• 化学式: C19H22BrNO3
• 分子量: 392.3
• InChiKey: KIAIFHTWTMKEDI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.91
• 重原子数：
  24
• 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：
  4
• 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。
• Combination of a dopamine D2-receptor agonist and tiotropium or a derivative therof for treating obstructive airways and other inflammatory diseases
  申请人：Yeadon Michael

  公开号：US20070117788A1

  公开（公告）日：2007-05-24

  The present invention relates to a combination of therapeutic agents useful in the treatment of obstructive airways and other inflammatory diseases comprising (I) a dopamine D2-receptor agonist that is therapeutically effective in the treatment of said diseases when administered by inhalation; together with (II) an anti-cholinergic agent consisting of a member selected from the group consisting of tiotropium and derivatives thereof that is therapeutically effective in the treatment of said diseases when administered by inhalation; as well as to a method of treating said obstructive airways and other inflammatory diseases comprising administering to said mammal by inhalation a therapeutically effective amount of said combination of therapeutic agents; and a pharmaceutical composition comprising a pharmaceutically acceptable carrier together with said combination of therapeutic agents; and a package containing a pharmaceutical composition for insertion into a device capable of simultaneous or sequential delivery of said pharmaceutical composition in the form of an aerosol or dry powder dispersion to said mammal, where said device is a metered dose inhaler or a dry powder inhaler. It is preferred that said dopamine D2-receptor agonist component be bromocriptine mesylate, naxagolide hydrochloride, cabergoline, pergolide mesylate, quinpirole hydrochloride, or ropinirole hydrochloride; and that said anti-cholinergic agent component be tiotropium bromide.
• METHODS FOR TREATING NEUROLOGICAL DISORDERS OR DAMAGE
  申请人：Tyers Mike

  公开号：US20090076019A1

  公开（公告）日：2009-03-19

  A clonogenic neurosphere assay is described that carries out high throughput screens (HTS) to identify potent and/or selective modulators of proliferation, differentiation and/or renewal of neural precursor cells, neural progenitor cells and/or self-renewing and multipotent neural stem cells (NSCs). Compositions comprising the identified modulators and methods of using the modulators and compositions, in particular to treat neurological disorders (e.g. brain or CNS cancer) or damage are also disclosed.
• US8058243B2
  申请人：——

  公开号：US8058243B2

  公开（公告）日：2011-11-15
• [EN] DOPAMINE AGONIST COMPOUNDS
  申请人：NORTHEASTERN UNIVERSITY

  公开号：WO1990012574A1

  公开（公告）日：1990-11-01

  (EN) Orally effective dopamine agonist compounds are described including in particular novel aporphine compounds. The compounds have a dioxy group on an aromatic nucleus which is cleaved in vivo to release compounds with two adjacent hydroxy groups on the aromatic nucleus. Also described are novel dopamine agonist aporphine compounds wherein the phenolic hydroxyl group is replaced by amino, bromo or fluoro groups.(FR) Sont décrits des composés agonistes de la dopamine efficaces oralement et notamment de nouveaux composés d'aporphine. Ces composés possèdent un groupe dioxy sur un noyau aromatique qui est clivé in-vivo pour libérer des composés présentant deux groupes hydroxy adjacents sur le noyau aromatique. Sont également décrits de nouveaux composés d'aporphine agonistes de la dopamine dans lesquels le groupe hydroxyl phénolique est remplacé par des groupes amino, bromo ou fluoro.