Disposition of [3H]flobufen and its active metabolite in rats

The present authors investigated the excretion, distribution and pharmacokinetics of the novel potential antirheumatic agent flobufen and its active metabolite after p.o. and i.v. doses of 2, 10 and 50 mg/kg administered to rats. The drug is resorbed well from the digestive tract and mostly it is metabolized to the principal metabolite M, which is only slowly excreted from the organism mainly by renal clearance. Within the whole dose range the kinetics of the drug is linear. Binding of flobufen and M to proteins is high (95-99%). The highest concentrations of radioactive metabolites (mostly M) were found in the plasma, liver, lungs, kidneys, connective tissue and inflammatory foci. The penetration of metabolites through the placenta and excretion in human milk are relatively important.     

Studies of the reproductive toxicity of Rumalaya

The reproductive toxicity of the complex plant preparation Rumalaya was studied in experiments on white mongrel rats. Rumalaya at doses of 400 and 2000 mg/kg given via the intragastric route with simultaneous application of cream to the skin was found to have no embryotoxic or teratogenic actions and had no significant effect on the postnatal development of offspring or the generative functions of female or male rats. Thus, these data identified no contraindications to the clinical use of this agent in pregnant women. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 41, No. 8, pp. 3–6, August, 2007.     

Potassium assay in blastomere of two-cell mouse embryo after equilibration and washing from cryoprotector

The need for effective methods of cryopreservation of early mammalian embryos necessitates the study of the mechanisms of blastomere adaptation to the equilibration procedure and subsequent washing from the cryoprotector. The osmotic effects during these procedures can cause electrolyte imbalance in embryonic cells. Intracellular potassium concentrations at the stage of two-blastomere mouse embryo were studied by electron probe microanalysis. Translated fromByulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 138, No. 7, pp. 48–49, July, 2004     

Synthesis and antioxidant activity of 3,5-dimethyl-4-hydroxybenzylthiododecane

The new multifunctional antioxidant 3,5-dimethyl-4-hydroxybenzylthiododecane (DHBD) demonstrated high activity both in vitro and in vivo. Experiments in vitro showed that the antioxidant activity of DHBD significantly exceeded that of the well-known reference drug ionol. A course of DHBD administration (100 mg/kg, p.o.) significantly decreased the content of lipid peroxidation products in rat brain on the model of long-term incomplete cerebral ischemia.     

Neurodevelopmental phenotype associated with CHD8-SUPT16H duplication

Microdeletions encompassing 14q11.2 locus, involving SUPT16H and CHD8, were shown to cause developmental delay, intellectual disability, autism spectrum disorders and macrocephaly. Variations leading to CHD8 haploinsufficiency or loss of function were also shown to lead to a similar phenotype. Recently, a 14q11.2 microduplication syndrome, encompassing CHD8 and SUPT16H, has been described, highlighting the importance of a tight control of at least CHD8 gene-dosage for a normal development. There have been only a few reports of 14q11.2 microduplications. Patients showed variable neurodevelopmental issues of variable severity. Breakpoints of the microduplications were non-recurrent, making interpretation of the CNV and determination of their clinical relevance difficult. Here, we report on two patients with 14q11.2 microduplication encompassing CHD8 and SUPT16H, one of whom had normal intelligence. Review of previous reports describing patients with comparable microduplications allowed for a more precise delineation of the condition and widening of the phenotypic spectrum.

     

Results, problems and perspectives of modern classification systems in psychiatry]

The new international classification of mental disorders (ICD 10) changes to a considerable extent the logical pattern, terminology and nomenclature of mental diseases. The prerequisite for its understanding is knowledge of general principles of medical classification and knowledge of basic theoretical problems associated with the classification of mental disorders. The paper summarizes these areas.