Psychiatry related information on l-Ketamine

• Plasma concentrations, maximum regional brain concentrations, and specific regional binding in the brain after administration of 0, 0.1, and 0.2 mg/kg doses of (S)-ketamine were measured in a randomized, double-blind, crossover study in five volunteers and were related to induced effects such as analgesia, amnesia, and mood changes [1].
• Current PTSD symptoms were substantially elevated in (S)-ketamine subjects, while there was no difference observed between opioids and racemic ketamines [2].
• Effects of different subanaesthetic doses of (S)-ketamine on psychopathology and binocular depth inversion in man [3].
• In spite of dose dependence and grave subjective and significant objective psychopathology, no significant impairment of binocular depth perception was found with (S)-ketamine [3].

High impact information on l-Ketamine

• Central nervous system effects of subdissociative doses of (S)-ketamine are related to plasma and brain concentrations measured with positron emission tomography in healthy volunteers [1].
• METHODS: Fifteen healthy volunteers were included in a double-blind, cross-over study with two doses of the serotonin 5-HT2A agonist DMT and the glutamate N-methyl-D-aspartate (NMDA) antagonist (S)-ketamine [4].
• Psychological effects of (S)-ketamine and N,N-dimethyltryptamine (DMT): a double-blind, cross-over study in healthy volunteers [4].
• CYP2B6 mainly mediates the N-demethylation of (R)- and (S)-ketamine in human liver microsomes at therapeutic concentrations (5 microM) [5].
• The kinetic data in human liver microsomes for the (R)- and (S)-ketamine N-demethylase activities could be analyzed as two-enzyme systems [5].

Biological context of l-Ketamine

• It was found that (S)-ketamine binds with a 3-4 time higher affinity to the PCP binding site of the NMDA receptor than (R)-ketamine, and that at these concentrations (R)-ketamine interacts also weakly with the sigma receptor sites, where (S)-ketamine binds only negligibly [6].
• Effects of different subanesthetic doses of (S)-ketamine on neuropsychology, psychopathology, and state of consciousness in man [7].

Anatomical context of l-Ketamine

• Psychotomimetic doses of (S)-ketamine increased cerebral metabolic rates of glucose (CMRglu) markedly in the frontal cortex including the anterior cingulate, parietal and left sensorimotor cortex, and in the thalamus [6].

Associations of l-Ketamine with other chemical compounds

• In contrast, (S)-ketamine was much weaker as an antagonist of 5-HT(3) receptors than NMDA receptors [8].
• METHODS: For corneal transplantation, all animals were intraperitoneally injected with 0.08 ml of a 1:8 mixture of 2% xylazine and 2.5% esketamine hydrochloride [9].

Analytical, diagnostic and therapeutic context of l-Ketamine

• The magnitude of specific binding of (S)-ketamine, measured with positron emission tomography, can be related directly to drug effects [1].

References