6 (R)-l-erythro-5,6,7,8-tetrahydrobiopterin receptor
    1.
    发明授权
    6 (R)-l-erythro-5,6,7,8-tetrahydrobiopterin receptor 失效
    6(R)-1-赤型-5,6,7,8-四氢生物喋呤受体

    公开(公告)号:US5606020A

    公开(公告)日:1997-02-25

    申请号:US87802

    申请日:1993-07-15

    CPC分类号: C07K14/705 A61K38/00

    摘要: A receptor (binding protein) specific for 6(R)-L-erythro-5,6,7,8-tetrahydrobiopterin which is a drug effective for neuropsychiatric disorders such as infantile autism is provided. This receptor is contained in the cytosol fraction or the membrane fraction obtained from a homogenate of an animal organ. It is solubilized from the membrane fraction in the presence of 3-{(3-cholamidopropyl)-dimethylammonio}-1-propanesulfonate (CHAPS). This receptor is characterized in that the binding ability thereof to 6R-BH4 is mostly lost by heating at 100.degree. C. for 10 minutes, the binding ability thereof to 6R-BH4 is significantly lost by incubating with trypsin at 37.degree. C. for 15 minutes, and said receptor shows a relative molecular weight of about 340 to 380 kilodaltons when specifically bound to tritium-labeled 6R-BH4 and analyzed with a molecular sieve provided with a COSMOSIL 5 Diol-300 column.

    摘要翻译: PCT No.PCT / JP92 / 01496 371日期:1993年7月15日 102(e)日期1993年7月15日PCT 1991年11月16日PCT PCT。 出版物WO92 / 10550 日期:1993年5月27日提供了对于作为神经精神障碍如婴儿自闭症有效的药物的6(R)-L-赤式-5,6,7,8-四氢生物喋呤特异性的受体(结合蛋白)。 该受体包含在细胞溶胶级分或从动物器官的匀浆获得的膜级分中。 在3 - {(3-胆酰胺基丙基) - 二甲基铵基}丙烷磺酸盐(CHAPS)存在下,从膜组分中溶解。 该受体的特征在于,通过在100℃下加热10分钟,其与6R-BH4的结合能力大部分丧失,通过用胰蛋白酶在37℃下孵育15分钟,6R-BH4的结合能力显着丧失 分钟,当与氚标记的6R-BH4特异性结合时,所述受体显示约340至380千道尔顿的相对分子量,并用配有COSMOSIL 5 Diol-300柱的分子筛分析。

    Isocarbacyclin derivatives
    7.
    发明授权
    Isocarbacyclin derivatives 失效
    异卡环素衍生物

    公开(公告)号:US5700833A

    公开(公告)日:1997-12-23

    申请号:US594152

    申请日:1996-01-31

    CPC分类号: C07C59/54

    摘要: The present invention provides novel isocarbacyclin derivatives useful for search and study of prostacyclin receptor and as a therapeutic drug for central nervous system diseases, which derivatives are expressed by the following formula �I!: ##STR1## �where, R.sup.1 represents a hydrogen atom, an alkyl group, or cation of an appropriate amount, and R.sup.2 an alkylene group.!

    摘要翻译: 本发明提供了可用于前列环素受体的研究和研究的新型异卡波环素衍生物,作为中枢神经系统疾病的治疗药物,该衍生物由下式[I]表示:其中,R1表示 氢原子,烷基或适当量的阳离子,R 2为亚烷基。

    METHOD FOR INTRODUCING DOTA
    9.
    发明申请
    METHOD FOR INTRODUCING DOTA 审中-公开
    引言DOTA的方法

    公开(公告)号:US20110237774A1

    公开(公告)日:2011-09-29

    申请号:US13123137

    申请日:2009-10-09

    IPC分类号: C07K1/113 C07H1/00

    摘要: The invention provides a method for introducing 1,4,7,10-tetraazacyclododecane-N,N′,N″,N′″-tetraacetic acid (DOTA) into a compound such as a peptide. The method comprises a first step for preparing a mixed liquid of DOTA having no protecting group and dimethylsulfoxide, and a second step for contacting the mixed liquid with the compound carried on a solid-phase carrier.

    摘要翻译: 本发明提供了将1,4,7,10-四氮杂环十二烷-N,N',N“,N” - 四乙酸(DOTA)引入化合物如肽中的方法。 该方法包括:制备没有保护基和二甲基亚砜的DOTA的混合液的第一步骤,以及使混合液与载持在固相载体上的化合物接触的第二步骤。