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Biomedical subjects

V P Shevchenko

Publications and source records attributed to V P Shevchenko.

At least 55 records · Page 3Linked to original sources
PubMedDate not supplied

[A synthesis of tritium-labeled olanzapine].

A synthesis of olanzapine, 2-methyl-10-(4-methyl-1-piperazinyl)-4H-thieno[2,3-b][1,5]benzodiazepine was carried out, and the conditions for its tritium labeling were optimized, to get a tritium-labeled olanzapine preparation with molar radioactivity of 12 Ci/mmol.

Benzodiazepines↗
PubMedDate not supplied

[Species and tissue distribution specificity of proteins binding 16alpha,17alpha-cycloalkane derivatives of progesterone].

The binding of [3H]progesterone and [3H] 16 alpha,17 alpha-cycloalkanoprogesterones to proteins from rat, rabbit, and human uteri and other organs was studied. We found that 16 alpha,17 alpha-cycloalkanoprogesterone derivatives display affinities for the uterine progesterone receptors comparable with that of the natural hormone and no substantial species differences in the affinity. Rabbit uterus was found to have no proteins distinct from the progesterone receptor that specifically bind [3H] 16 alpha,17 alpha-cycloalkanoprogesterones. At the same time, in the human uterus, we found another protein that binds some of these progesterone derivatives; it turned out to be similar to the protein from rat uterus. A similar protein with the same selectivity and affinity for steroids was also found in rat and human kidneys. Blood serum, liver, lung, and a number of other tissues were found to contain a protein of the third type that binds the same 16 alpha,17 alpha-cycloalkanoprogesterones and exhibits submicromolar Kd values for these steroids and a very low affinity for progesterone. We speculated that the introduction of a bulky substituent adjacently to the 17 beta-side chain of progesterone could result in a change in the general biodynamics of the derivative including its transport, uptake, and accumulation in tissues, which may determine the selectivity of its effect.

Animals↗
PubMedDate not supplied

[Kinetics of Semax penetration into the brain and blood of rats after its intranasal administration].

The radioactive peptide analogue Semax corresponding to the ACTH(4-10) sequence (Met-Glu-His-Phe-Pro-Gly-Pro) with a molar radioactivity of 56 Ci/mmol labeled with tritium at the C-terminal Pro was prepared. The labeled peptide was used for studying the kinetics of Semax penetration into rat brain and blood after its intranasal administration (50 microg/kg, 20 microl of solution) to nonbred white rats of body mass 200-250 g. It was demonstrated that 0.093% of the total introduced radioactivity per gram can be found in the rat brain 2 min after the administration, 80% of this radioactivity belonged to Semax, and the rest, to its metabolites. The peptide undergoes rapid enzymatic degradation, with the tripeptide Pro-Gly-Pro prevailing in biological samples relative to the total content of Semax and its metabolites.

Administration, Intranasal↗
PubMedDate not supplied

[Arachidonoyl amino acids and arachidonoyl peptides: synthesis and properties].

N-Arachidonoyl (AA) derivatives of amino acids (glycine, phenylalanine, proline, valine, gamma-amino butyric acid (GABA), dihydroxyphenylalanine, tyrosine, tryptophan, and alanine) and peptides (Semax, MEHFPGP, and PGP) were synthesized in order to study the biological properties of acylamino acids. The mass spectra of all the compounds at atmospheric pressure electrospray ionization display the most intense peaks of protonated molecular ions; the detection limits for these compounds are 10 fmol per sample. AA-Gly showed the highest inhibitory activity toward fatty acid amide hydrolase from rat brain (IC50 6.5 microM) among all the acylamino acids studied. AA-Phe, AA-Tyr, and AA-GABA exhibited a weak but detectable inhibitory effect (IC50 55, 60, and 50 microM, respectively). The acylated amino acids themselves, except for AA-Gly, were stable to the hydrolysis by this enzyme. All the arachidonoylamino acids inhibited cabbage phospholipase D to various degrees; AA-GABA and AA-Phe proved to be the most active (IC50 20 and 27 microM, respectively). Attempts to detect the biosynthesis of AA-Tyr in homogenates of rat liver and nerve tissue showed no formation in vitro of either this acylamino acid or AA-dopamine and AA-Phe, the products of its metabolism. The highest contents of these metabolites were detected in liver homogenate and in the brain homogenate, respectively. Acylamino acids exert no cytotoxic effect toward the glioma C6 cells. It was shown that N-acylation of Semax with arachidonic acid results in enhancement of its hydrolytic stability and increases its affinity for the sites of specific binding in rat cerebellum membranes. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2006, vol. 32, no. 3; see also http://www.maik.ru.

Amino Acids↗
PubMedDate not supplied

[Morphological changes in the rat uterine tissues exposed to pregna-D'-pentaran derivatives of progestins and anti-progestins].

Changes in the uterus morphology of mature female rats were studied on the model of pseudopregnancy after treatment with the progestin 16 alpha,17 alpha-cyclohexanoprogesterone (PR) and the antirpogestins 5 alpha(H)-16 alpha,17 alpha-cyclohexano-4,5-dihydroprogesterone (APR1) and 5 beta(H)-16 alpha,17 alpha-cyclohexano-4,5-dihydroprogesterone (APR2). The rats were preliminarily estrogenized with 17 beta-estradiol at a dose of 1 microgram/(animal day) for 4 days and then treated with PR at a dose of 0.2 mg/(animal day) for 14 days. The first group was then left without any treatment, whereas APR1 and APR2 were injected at the dose of 0.2 mg/(animal day) for 4 days to the animals of the second and the third groups, respectively. Light and electron microscopy of the uterus preparations demonstrated that the PR action provoked a complete pseudopregnancy picture characterized by the endometrium functionalization and the myometrium hypertrophy. Subsequent treatment with APR1 and APR2 caused the hypertrophy to cease, which had a more pronounced effect in the case of APR1. At the same time, some indications of the endometrium functionalization remained observable after treatment with APR1 and APR2. The specific binding sites for 3H-labeled APR1 and APR2 were absent from the uterus cytosol for the rats gestagenized with PR.

Animals↗
PubMedDate not supplied

[Secondary autoimmune syndrome and immunomodulating lymphotropic therapy in acute pancreatitis].

Immune status and condition of regional lymphoid tissue were studied in 28 patients with various forms of acute pancreatitis untreated with immunomodulating therapy and in 12 patients receiving combined therapy including lymphotropic regional therapy with T-activin. Acute pancreatitis patients were found to have aquired immunodeficiency, secondary autoimmune syndrome and reaction of toxic immune complexes the severity of which decreased under the action of T-activin therapy.

Adjuvants, Immunologic↗
PubMedDate not supplied

[Electroencephalography monitoring at total and managed hyperthermia to 44 degrees C].

In 34 patients the abstinence syndrome was treated by hypothermia (HT) with the EEG monitoring. HT was carried out under the general propofol-fentanil anesthesia. HT was achieved in the "Hirana" bath. The temperature was increased gradually by 1 degree C per 5 minutes up to 44 degrees C. EEG was recorded before anesthesia, as well as during and after the procedure. On the initial EEG alpha- and beta-rhythms were predominant. Under the anesthesia both alpha-rhythm frequency and amplitude were enhanced, spikes and wave discharges appeared. Under HT (t = 40-42 degrees C) low voltage and wave slowing were recorded. In the range t degree--42.5-43.4 degrees C EEG registered the appearance of clinically significant "biological break point", which was followed by neuropeptide destruction. At t degree--43-44 degrees C acute suppression and, then, electrocerebral silence were observed in a majority of patients. At the end of the procedure (t = 39 degrees C) EEG returned to the initial recording.

Anesthesia, General↗
PubMedDate not supplied

[Early nutrition support for intestinal insufficiency syndrome in spine surgery].

Paresis of the gastrointestinal tract resulting in the intestinal insufficiency syndrome (IIS) is a postoperative risk factor in spinal surgery. One hundred and twenty patients with fractures at L1-L2 spine level, isthmic spondylolisthesis, osteochondrosis and with sever neurological symptoms were examined and treated. The intestinal motor-evacuation malfunction, hypermetabolism, microbial translocation and immunity impairments are observed in IIS. Early nutritional support is indicated for the IIS prevention and treatment. Enteral feeding with new balanced mixtures containing fibers is effective.

Adult↗
PubMedDate not supplied

[Some pathophysiological aspects of hyperthermic pharmacotherapy and its clinical use].

The use of artificially induced general controllable hyperthermia (GCH) of high degree is acknowledged as the 21st century intensive technology; it is used in the treatment of diseases and conditions that can be hardly cured by routine methods. Pathogenetic pharmacotherapy was made use of to enhance, purposefully, the GCH efficiency. The suggested concept, i.e. reproduction of the most efficient use of positive effects from high temperature and thermally mediated effects of pharmacotherapy, was named as "hyperthermic pharmacotherapy". The controllable maintenance of the "biological zero" phenomenon in the brain (registered by EEG) at 42-44 degrees C is the safety criterion of high-level GCH. The described intensive-care technique can be referred to as promising considering the modern anesthesiological-management potentialities related with GCH safety.

Brain↗