2.alpha., 3.beta., 4a.beta.,
8a.alpha.-Decahydro-3-(4-phenyl-1-piperidinyl)-2-naphthalenol
    2.
    发明授权
    2.alpha., 3.beta., 4a.beta., 8a.alpha.-Decahydro-3-(4-phenyl-1-piperidinyl)-2-naphthalenol 失效
    2α,3β,4aβ,8aα-十氢-3-(4-苯基-1-哌啶基)-2-萘酚

    公开(公告)号:US4552965A

    公开(公告)日:1985-11-12

    申请号:US636183

    申请日:1984-07-31

    CPC classification number: C07D211/14

    Abstract: A compound denominated (2.alpha., 3.beta., 4a.beta., 8a.alpha.)-decahydro-3-(4-phenyl-1-piperidinyl)-2-naphthalenol(DPPN) having the following chemical structure: ##STR1## DPPN is more effective than other known compounds in blocking presynaptic release of acetylcholine at cholinergic synapses.

    Abstract translation: 具有以下化学结构的化合物(2α,3β,4aβ,8aαα) - 十氢-3-(4-苯基-1-哌啶基)-2-萘酚(DPPN)更有效 比其他已知的化合物在胆碱能突触中阻断乙酰胆碱的突触前释放。

    Methods, compositions and apparatuses for detection of gamma-hydroxybutyric acid (GHB)
    8.
    发明授权
    Methods, compositions and apparatuses for detection of gamma-hydroxybutyric acid (GHB) 有权
    用于检测γ-羟基丁酸(GHB)的方法,组合物和装置

    公开(公告)号:US06703216B2

    公开(公告)日:2004-03-09

    申请号:US10098811

    申请日:2002-03-14

    Abstract: Methods, compositions and articles of manufacture for assaying a sample for a GHB source are provided. A sample suspected of containing a GHB source is contacted with a first oxidoreductase selective for GHB and an oxidized cofactor. In the presence of GHB in the sample, the first oxidoreductase oxidizes GHB to succinic semialdehyde and reduces the cofactor. The reduced cofactor thus produced can be detected directly, or a hydride abstractor can be used that abstracts a hydride from the reduced cofactor and produces a detectable change. The hydride abstractor can be a second oxidoreductase that oxidizes the reduced cofactor and produces a detectable change in a chromogen or dye. Preferably a visual change is produced, allowing performance of the assay outside of a laboratory setting. Fusion proteins comprising the first oxidoreductase, polynucleotides encoding such proteins, host cells expressing such proteins, and vectors comprising such polynucleotides are also provided. Stabilized formulations of the first oxidoreductase are also provided. Test supports, devices, and compositions and kits comprising reagents for performing such methods are also provided. Techniques for performing the assay in the presence of ethanol and in the presence of GHB precursors in the sample are also provided.

    Abstract translation: 提供了用于测定GHB源的样品的方法,组合物和制品。 怀疑含有GHB来源的样品与GHB和氧化辅因子选择性的第一氧化还原酶接触。 在样品中存在GHB时,第一氧化还原酶将GHB氧化成琥珀酸半醛,并减少辅因子。 可以直接检测如此产生的还原辅因子,或者可以使用从还原辅因子中提取氢化物并产生可检测变化的氢化物提取器。 氢化物提取器可以是氧化还原的辅因子并在色原体或染料中产生可检测的变化的第二氧化还原酶。 优选地,产生视觉变化,允许在实验室设置之外执行测定。 还提供了包含第一氧化还原酶,编码这种蛋白质的多核苷酸,表达这种蛋白质的宿主细胞和包含这种多核苷酸的载体的融合蛋白质。 还提供了第一氧化还原酶的稳定制剂。 还提供了测试载体,装置和包含用于执行这些方法的试剂的组合物和试剂盒。 还提供了在乙醇存在下和样品中GHB前体存在下进行测定的技术。

    Spirovesamicols
    10.
    发明授权
    Spirovesamicols 失效
    螺环素

    公开(公告)号:US5457207A

    公开(公告)日:1995-10-10

    申请号:US131887

    申请日:1993-10-05

    CPC classification number: A61K51/0457 C07D221/20 C07D401/04 A61K2123/00

    Abstract: The compounds are vesamicol (hydroxylated phencyclidine (PCP) isomer trans-2-(4-phenyl-piperidino)cyclohexanol) derivatives with anticholinergic properties termed herein "spirovesamicols" which are spirofused piperidines. The compounds bind to the vesamicol receptor, a site on the cholinergic synaptic vesicle, which is associated with the vesicular transporter of acetylcholine.

    Abstract translation: 这些化合物是具有抗胆碱能特性的称为本文中称为螺旋体哌啶的“螺环胺”的维生素(羟基化苯环利定(PCP)异构体反式-2-(4-苯基 - 哌啶子基)环己醇)衍生物。 这些化合物与乙酰胆碱受体结合,胆碱能突触小泡的一个位点与乙酰胆碱的水泡转运蛋白有关。

Patent Agency Ranking