Synthesis and benzodiazepine receptors affinity of 2,3-dihydro-9-phenyl-1H-pyrrolo[3,4-b]quinolin-1-one and 3-carbethoxy-4-phenylquinoline derivatives

A series of 2,3-dihydro-9-phenyl-1H-pyrrolo[3,4-b]quinolin-1-one derivatives and related compounds were tested for their ability to bind benzodiazepine receptors (BZRs). Most of the synthesized compounds showed micromolar affinity for BZR peripheral type, but not for the central one, with the except...

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Published inFarmaco (Società chimica italiana : 1989) Vol. 47; no. 2; p. 191
Main Authors Anzini, M, Cappelli, A, Vomero, S, Cagnotto, A, Skorupska, M
Format Journal Article
LanguageEnglish
Published France 01.02.1992
Subjects
Animals
Brain Chemistry - drug effects
In Vitro Techniques
Mice
Mice, Inbred Strains
Pyrroles - chemical synthesis
Pyrroles - pharmacology
Quinolones - chemical synthesis
Quinolones - pharmacology
Rats
Receptors, GABA-A - drug effects
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Summary:A series of 2,3-dihydro-9-phenyl-1H-pyrrolo[3,4-b]quinolin-1-one derivatives and related compounds were tested for their ability to bind benzodiazepine receptors (BZRs). Most of the synthesized compounds showed micromolar affinity for BZR peripheral type, but not for the central one, with the exception of compound 4m which displayed an IC50 = 0.407 microM, only 2 fold higher than IC50 for chlordiazepoxide.
ISSN:0014-827X