Melani F, Cecchi L, Colotta V, Filacchioni G, Martini C, Giannaccini G, Lucacchini A
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
Farmaco. 1989 Jun;44(6):585-94.
Some 2,6,8-trisubstituted dipyrazolo[5,4-b:3',4'-d]pyridin-3-ones related to the CGS series were synthesized and tested for their ability to displace [3H]flunitrazepam binding from bovine brain membranes. However the affinity for the benzodiazepine receptor of the tested compounds was lower than that of the CGS series, although it was comparable to that of chlordiazepoxide. It follows that some structure-activity relationships on the tested compounds can be drawn.
合成了一些与CGS系列相关的2,6,8-三取代二吡唑并[5,4-b:3',4'-d]吡啶-3-酮,并测试了它们从牛脑膜中取代[3H]氟硝西泮结合的能力。然而,尽管测试化合物对苯二氮卓受体的亲和力与氯氮卓相当,但低于CGS系列。由此可以得出一些关于测试化合物的构效关系。