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新型6H-吲哚并[2,3-b][1,8]萘啶的合成及其对苯二氮䓬受体的特异性抑制作用。

Synthesis of new 6H-indolo[2,3-b] [1,8]naphthyridines and their specific inhibition of benzodiazepine receptor.

作者信息

Da Settimo A, Primofiore G, Ferrarini P L, Mori C, Martini C, Pennacchi E, Lucacchini A

出版信息

Farmaco Sci. 1986 Aug;41(8):577-85.

PMID:3017748
Abstract

Some 3-amino- and 3-hydroxy-8-halosubstituted 6H-indolo[2,3-b] [1,8]naphthyridines were synthesized and tested for their affinity for the benzodiazepine receptor in bovine cortical membranes. All prepared compounds were more active than the corresponding 8-unsubstituted derivatives. Moreover, among these compounds the 8-chloroindolonaphthyridines were clearly the most potent.

摘要

合成了一些3-氨基和3-羟基-8-卤代取代的6H-吲哚并[2,3-b][1,8]萘啶,并测试了它们对牛脑皮层膜中苯二氮䓬受体的亲和力。所有制备的化合物都比相应的8-未取代衍生物更具活性。此外,在这些化合物中,8-氯吲哚萘啶显然是最有效的。

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