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PREPARATION OF STEROID SULFAMATES AND THEIR INTERACTION WITH GABA^sub A^ RECEPTOR

机译:甾体硫酸盐的制备及其与GABA ^ sub A ^受体的相互作用

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Sulfamoyl chloride was used for the preparation of 3α- and 3β-sulfamates of steroids: 20-oxo-5α-pregnan-3α-yl sulfamate (4), 20-oxo-5α-pregnan-3β-yl sulfamate (5), 20-oxo5β-pregnan-3α-yl sulfamate (7), and 20-oxo-5β-pregnan-3β-yl sulfamate (9) from the corresponding 3α- and 3β-alcohols. Sulfur trioxide-pyridine complex was employed for the preparation of 20-oxo-5α-pregnan-3α-yl pyridinium sulfate (10). The specific steroid binding was detected by the decrease of the specific [^sup 35^S]-tert-butylbicyclo[2.2.2]phosphorothionate binding after application of the tested compounds. [PUBLICATION ABSTRACT]
机译:氨磺酰氯用于制备甾族化合物的3α-和3β-氨基磺酸酯:20-氧代-5α-pregnan-3α-氨基磺酸酯(4),20-氧代-5α-pregnan-3β-氨基磺酸酯(5),20 -oxo5β-pregnan-3α-氨基磺酸酯(7)和20-oxo-5β-pregnan-3β-氨基磺酸酯(9)来自相应的3α-和3β-醇。用三氧化硫-吡啶配合物制备20-氧代-5α-pregnan-3α-基吡啶鎓硫酸盐(10)。在施用受试化合物后,通过减少特定的[s 35 ter]-叔丁基双环[2.2.2]磷酸硫代酸酯结合来检测特异性的类固醇结合。 [出版物摘要]

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    VOJTECH KAPRAS1, EVA STASTNÁ2, HANA CHODOUNSKÁ3'*, VLADIMÍR POUZAR4 andZdena KRISTOFÍKOVÁ5Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i.,CZ-166 10 Prague 6, Czech Republic, e-mail: 1 kapras@uochb. cas.cz, 2 stastna@uochb.cas.cz,3 hchod@uochb.cas.cz, 4 pouzar@uochb.cas.cz, 5 kristofikova@pcp.lf3.cuni.czReceived September 12, 2008Accepted March 11, 2009Published online April 6, 2009,;

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