New Journal of Chemistry
January 1, 2018
Bronislav Jurásek, František Králík, Silvie Rimpelová et al.
15 citations
The dissociative drug deschloroketamine was synthesized, and the absolute configuration of its enantiomers was determined. The in vitro cytotoxicity of each enantiomer was tested across nine different cell lines, providing data on their relative toxicities.
British journal of pharmacology
January 1, 2022
Kristýna Štefková-mazochová, Hynek Danda, Wim Dehaen et al.
13 citations
Deschloroketamine (DCK), a structural analogue of ketamine sold as a recreational drug, was tested in Wistar rats to examine its pharmacokinetics, acute effects, and addictive potential. DCK rapidly entered the brain, with peak levels at 30 minutes and sustained high levels for 2 hours. It blocks NMDA receptors similarly to ketamine, with the S-enantiomer more potent. DCK stimulated locomotion, induced place preference (a sign of reward), and strongly disrupted prepulse inhibition (PPI). Locomotor stimulation faded faster than PPI disruption. S-DCK had stronger stimulatory effects than R-DCK, but both equally disrupted PPI. DCK's behavioral and addictive profiles resemble ketamine's, with a slightly slower clearance, matching its reported longer duration. These findings clarify risks of illicit DCK use.
Pharmaceuticals
November 30, 2022
Martin Paškan, Silvie Rimpelová, Vladimíra Svobodová Pavlíčková et al.
9 citations
A novel synthetic cathinone, 4-isobutylmethcathinone, was synthesized and its properties characterized. The substance showed significantly higher cytotoxicity compared to other synthetic cathinones, with IC50 values reaching 18–65 µM after 72 hours in human bladder, neuroblastoma, microglia, and liver cancer cells. Chiral separation enabled study of individual enantiomers, which exhibited different agonistic effects on dopamine and adrenergic receptors. The compound lacked binding affinity for serotonin receptors, placing it among monoamine drugs like MDMA.
New Journal of Chemistry
January 1, 2023
Bronislav Jurásek, Patrik Fagan, Bohumil Dolenský et al.
6 citations
Methoxphenidine, a dissociative anesthetic related to phencyclidine, was originally patented for its potential to treat neurotoxic injury. The abstract indicates that the compound was developed with therapeutic applications in mind, specifically for addressing damage to the nervous system. No further details about its efficacy, mechanism, or clinical use are provided in this text.
Powder Diffraction
June 21, 2017
J. Maixner, Bronislav Jurásek, Michal Kohout et al.
5 citations
The crystal structure of S-2-(methylamino)-2-phenylcyclohexan-1-one hydrochloride (C13H18ClNO) was determined using X-ray powder diffraction. The compound crystallizes in the monoclinic space group P21 with unit-cell parameters a = 6.578 Å, b = 13.250 Å, c = 15.096 Å, β = 91.619°, and a unit-cell volume of 1315 ų, with four formula units per cell. All measured diffraction lines were indexed and are consistent with the assigned space group, and no detectable impurities were observed in the sample.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences
June 1, 2025
Natalie Paškanová, Magdaléna Vágnerová, Bronislav Jurásek et al.
1 citation
Methoxphenidine (MXP), a dissociative anaesthetic derivative, is increasingly abused, but forensic and clinical data on its metabolism and enantiomers are limited. Researchers developed and validated achiral LC-MS/MS and chiral SFC-MS methods to quantify MXP and its primary metabolite, O-desmethyl-methoxphenidine (dmMXP), in rat serum and brain after a single subcutaneous dose of racemic MXP. Serum MXP peaked at 1600 ng/mL at 0.5 hours and decreased to 5.87 ng/mL at 24 hours; brain MXP peaked at 13200 ng/g at 0.5 hours and fell to 36.1 ng/g at 24 hours. (S)-MXP concentrations in brain appeared higher than (R)-enantiomer concentrations. The methods enable pharmacokinetic studies and provide tools for forensic and clinical toxicology.