Chiral 1,4-benzodiazepin-2-ones: relationship between stereochemistry and pharmacological activity.

Salvadori, P; Bertucci, C; Domenici, E; Giannaccini, G

Salvadori, P; Bertucci, C; Domenici, E; Giannaccini, G.

Afiliación

Salvadori P; Centro di Studio del CNR per le Macromolecole Stereordinate Otticamente Attive, Dipartimento di Chimica e Chimica Industriale, Pisa, Italy.

J Pharm Biomed Anal ; 7(12): 1735-42, 1989.

Article en En | MEDLINE | ID: mdl-2562315

ABSTRACT

ABSTRACT

Pure enantiomers of 3-substituted-1,4-benzodiazepin-2-ones, obtained by HPLC resolution on chiral stationary phases, show significant differences in their pharmacological activity. The occurrence of biotransformation during the pharmacological test is monitored using a new chromatographic method. The reliability of the pharmacological activity data is discussed.

Asunto(s)

Benzodiazepinonas/química; Animales; Benzodiazepinonas/farmacología; Unión Competitiva/efectos de los fármacos; Biotransformación; Encéfalo/metabolismo; Bovinos; Dicroismo Circular; Flunitrazepam/metabolismo; Hidrólisis; Técnicas In Vitro; Membranas/metabolismo; Conformación Molecular; Receptores de GABA-A/efectos de los fármacos; Espectrofotometría Ultravioleta; Estereoisomerismo; Sinaptosomas/efectos de los fármacos; Sinaptosomas/metabolismo

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Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Benzodiazepinonas Límite: Animals Idioma: En Revista: J Pharm Biomed Anal Año: 1989 Tipo del documento: Article País de afiliación: Italia

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