[The effect of gamma rays on medazepam in a methanolic solution].

Nine radiolytical products have been identified in a methanolic solution of Medazepam exposed to gamma-irradiation. A decomposition model taking into account these radiolytical products is presented. The formation of the individual radiolytical products can be deduced from analogous reactions of the radicals e-sdv.

A PCILO study of the pharmacologically active conformation of local anesthetics of the procaine type. Conformational analysis and complex formation of protonated 2-diethylaminoethyl-acetate with formate anion.

To rationalize and improve receptor selectivity of local anesthetics of the procaine type a dynamic two-center model of the pharmacon-receptor interaction is suggested. A quantum chemical study within the Perturbation Configuration Interaction using Localized Orbitals (PCILO) approximations is carried out to find indications for a conformational change of this flexible drug from its thermodynamically preferred conformation to its pharmacologically active one. For this purpose, the pharmacon-receptor interaction is simulated quantum chemically by the interaction of the local anesthetic model compound 2-diethylaminoethyl-acetate (acetylcaine) with the one-center receptor model formate anion and the two-center receptor model gamma-aminobutyric acid in its zwitterionic form.

[Structure-activity relationships of analgesics].

With morphine or codeine derivatives and different classes of synthetic compounds (pethidine, methadone, morphinane, benzomorphinane, etc.) there are correlations between structure and analgesic effects on the basis of common structural elements. Such findings can be helpful in obtaining information about the effects of different receptors and help to explain their mode of action.