Synthesis of 1,5-diaryl-3-methyl-1H-pyrazolo[4,5-c]isoquinolines and studies of binding to specific peripheral benzodiazepine binding sites.

Synthesis of 1,5-diaryl-3-methyl-1H-pyrazolo[4,5-c]isoquinolines and studies of binding to specific peripheral benzodiazepine binding sites.
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DOI:
10.1002/jps.2600780602
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发表时间:
1989-06
影响因子:
3.8
通讯作者:
L. Cecchi;V. Colotta;F. Melani;G. Palazzino;G. Filacchioni;C. Martini;G. Giannaccini;A. Lucacchini
L. Cecchi;V. Colotta;F. Melani;G. Palazzino;G. Filacchioni;C. Martini;G. Giannaccini;A. Lucacchini
中科院分区:
医学3区
文献类型:
--
作者:
L. Cecchi;V. Colotta;F. Melani;G. Palazzino;G. Filacchioni;C. Martini;G. Giannaccini;A. Lucacchini

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合成了一些1,5-二芳基-3-甲基-1H-吡唑并[4,5-c]异喹啉类化合物,并测试了它们取代[3 H]氯硝西泮或[3 H]Ro 5-4864与中枢和外周苯二氮卓受体特异性结合的能力。没有测试的化合物显示任何活性作为中央结合抑制剂,而它们中的大多数是特异性作为外周结合抑制剂,虽然它们不是非常有效的。
Some 1,5-diaryl-3-methyl-1H-pyrazolo[4,5-c]isoquinolines were synthesized and tested for their ability to displace [3H]clonazepam or [3H]Ro 5-4864 from their specific binding on the central and peripheral benzodiazepine receptors. None of the tested compounds showed any activity as central binding inhibitors, while most of them were specific as peripheral binding inhibitors, although they were not very potent.