Savini L, Massarelli P, Corti P, Pellerano C, Bruni G, Romeo M R
Dipartimento Farmaco Chimico Technologico, Facoltà di Farmacia-Università, Siena, Italy.
Farmaco. 1993 Dec;48(12):1675-86.
Two new series of 2-arylpyrazolo[4,3-c]quinolin-3-ones (6,8-difluoro- and 7,9-dichloro-derivatives) have been synthesized and tested for their ability to displace [3H]flunitrazepam from rat brain membranes. Several compounds possess comparable and sometimes higher affinity for central benzodiazepine receptors than that of diazepam. Some selected compounds were also tested in vivo in the anti-pentylenetetrazol test; some anticonvulsant activity resulted for the 6,8-difluoroderivatives only.
已合成了两个新系列的2-芳基吡唑并[4,3-c]喹啉-3-酮（6,8-二氟和7,9-二氯衍生物），并测试了它们从大鼠脑膜中置换[3H]氟硝西泮的能力。几种化合物对中枢苯二氮䓬受体的亲和力与地西泮相当，有时甚至更高。还在体内戊四氮试验中对一些选定的化合物进行了测试；仅6,8-二氟衍生物产生了一些抗惊厥活性。
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