Detail of "33795-24-3"

Reference

On the pharmacology of the ketamine enantiomorphs in the rat

On the pharmacology of the ketamine enantiomorphs in the rat. Marietta, Michael P.; Way, Walter L.; Castagnoli, Neal, Jr.; Trevor, Anthony J. (Dep. Pharmacol., Univ. California, San Francisco, Calif., USA). J. Pharmacol. Exp. Ther., 202(1), 157-65 (English) 1977. CODEN: JPETAB. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Four pharmacol. effects (hypnosis, ataxia, locomotor activity and lethality), brain and plasma pharmacokinetic profiles and the in vitro hepatic metab. of racemic ketamine-HCl (I-HCl) [1867-66-9] and its 2 optical somers were studied in male, Sprrague-Dawley rats. At equimolar doses, the (+)-isomer [33795-24-3] elicited periods of hypnosis and ataxia nearly twice those of the (-)-isomer [33643-47-9]. No significant differences were obsd. between the brain and plasma levels of either isomers or I after equimolar administration (30 mg/kg). Obsd. differences in the rates of the in vitro hepatic metab. of the enantiomorphs did not appear to play an important role in the in vivo disposition of the isomers. From correlations between brain levels and pharmacol. activities, and estn. of ED50 values (hypnosis), differences in the hypnotic potencies of the isomers appeared to have a pharmacodynamic rather than a pharmocokinetic basis. After the administration of equihypnotic doses of the isomers, the posthypnotic stimulation of locomotor activity by the (+)-enantiomorph was significantly less intense than that of (-)-isomer. In addn., the therapeutic index (hypnosis) of the (+)-isomer (10.0), was greater than that of I (6.25) or the (-)isomer (4.0). These results suggest that the (+)-isomer may provide anesthesia which is safer and has fewer posthypnotic side effects when administered at dosages equihypnotic to those of I or its (-)-isomer.