苯二氮卓类受体配体。6-芳基-3,8-二取代-1,2,4-三唑[3,4-a]酞嗪的合成及药理评价。

G. Tarzia, E. Occelli, D. Barone
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引用次数: 0

摘要

以合适的邻苯甲酰苯甲酸为起始原料,合成了一系列6-芳基-3,8-二取代-1,2,4-三唑[3,4- A]邻苯二甲酸。在体外测试了化合物对大鼠脑突触体膜制备中3h -地西泮与苯二氮卓受体特异性结合的抑制作用。在这项试验中,这些化合物都没有明显的活性。
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Benzodiazepine receptor ligands. Synthesis and pharmacological evaluation of 6-aryl-3,8-disubstituted-1,2,4-triazolo[3,4-a]phthalazines.
A series of 6-aryl-3,8-disubstituted-1,2,4-triazolo[3,4-a]phthalazines was synthesised starting from suitable o-benzoylbenzoic acids. The compounds were tested in vitro for inhibition of the specific binding of 3H-Diazepam to benzodiazepine receptors in preparations of membranes from rat brain synaptosomes. None of the compounds was notably active in this test.
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