RESUMO
1. Five oxazolidines were synthesized by reaction of (-) ephedrine with formaldehyde, propionaldehyde, butyraldehyde, isobutyraldehyde, and acetone, respectively. 2. Half-lives of hydrolysis were measured in pH 7.4 aqueous buffer. Half-lives varied from 12 seconds to 11 minutes. 3. The compounds were evaluated for their ability to increase locomotor activity in rats. All compounds significantly increased locomotor activity at 50 mg/kg dose. 4. The formaldehyde derivative had similar activity to (-) ephedrine. All other compounds were less active than (-) ephedrine.
Assuntos
Estimulantes do Sistema Nervoso Central/farmacologia , Efedrina/farmacologia , Atividade Motora/efeitos dos fármacos , Pró-Fármacos/farmacologia , Animais , Relação Dose-Resposta a Droga , Meia-Vida , Masculino , Ratos , Ratos Sprague-DawleyRESUMO
1. The four stereoisomeric ephedrines and four oxazolidines formed by reaction of each ephedrine isomer with salicylaldehyde were tested for their ability to increase locomotor activity in rats. 2. All ephedrine isomers except (-)pseudoephedrine increased locomotor activity; the order of potency was (-)ephedrine > (+) pseudoephedrine > (+) ephedrine. 3. All oxazolidine derivatives increased locomotor activity except (-)pseudoephedrine oxazolidine. 4. The oxazolidines derived from (-) and (+) ephedrine were slightly more active than their parent drugs. (+) Pseudoephedrine oxazolidine was less active than its parent. 5. Half-lives of hydrolysis were measured for the oxazolidines in aqueous buffer, ephedrine oxazolidines hydrolyze faster than pseudoephedrine oxazolidines.
