European Journal of Medicinal Chemistry p. 859 - 868 (1995)
Update date:2022-08-04
Topics:
Tanaka, H.
Kirihara, S
Yasumatsu, H.
Yakushiji, T.
Nakao, T.
A series of 2-(4-chlorophenyl)-5,6-dihydrothieno<2'3':2,3>thiepino<4,5-c>pyridazin-3(2H)-ones were synthesized and evaluated in vitro for their affinity toward benzodiazepine receptors (BZRs) in rats and for their intrinsic efficacy in the augmentation of the γ-aminobutyric acid (GABA)-induced chloride currents in the dissociated frog sensory neurons.Compounds in wich the 9-position of the condensed-ring system was substituted with alkyl group or bromine had a high affinity toward BZRs.The substituents at the same position also influenced significantly the GABA-induced chloride currents.As the result, 9-alkyl and 9-bromo substutuents would interact with the lipophilic area of BZRs.A series of 2-(4-chlorophenyl)-5,6-dihydrothieno<2',3':2,3>thiepino<4,5-c>pyridazin-3(2H)-ones exhibited partial and full agonistic activities toward BZRs. benzodiazepine receptor / γ-aminobutyric acid / partial agonist / full agonist / structure activity relationship
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