76 results match your criteria: "Institute of Physiologically Active Substances[Affiliation]"

Phosphoryl podands of neutral type with a flexible ethylene glycol chain and diphenylphosphorylmethyl end groups are known for their complexation properties towards various cations. In this work, the complexation process between 1,3-bis(diphenylphosphoryl)-2-oxapropane (L) and lanthanide ions was studied. Namely, the stability constants of lanthanide complexes with L in acetonitrile were estimated by the method of spectrophotometric titration.

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Analysis of Natural Antibodies during the Development of Phantom Pain Syndrome.

Dokl Biochem Biophys

August 2024

Institute of Physiologically Active Substances, Federal Research Center for Problems of Chemical Physics and Medical Chemistry, Russian Academy of Sciences, Chernogolovka, Moscow oblast, Russia.

We determined natural antibodies (n-Abs) to the regulators of the main systems of biochemical homeostasis: β-endorphin, serotonin, dopamine, histamine, orphanin, angiotensin, GABA, glutamate, bradykinin, vasopressin, thrombin, and α-2-macroglobulin in individuals with phantom pain syndrome (PPS), resulting from amputation after injury. It was established that each patient has an individual immunoprofile, but for all of them there was a significant increase in the level of antibodies to serotonin, histamine, and angiotensin, which reflect the chronicity of the pain syndrome and do not depend on the self-assessment of the severity of PPS. Determination of the role of regulators of biochemical homeostasis in the development of phantom pain showed that, at high, moderate, and weak severity of PPS, the biogenic amine and angiotensinergic systems are activated.

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New Hybrid Structures Based on Memanthine and Edaravone Molecules.

Dokl Biochem Biophys

October 2023

Institute of Physiologically Active Substances, Federal Research Center for Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Chernogolovka, Moscow oblast, Russia.

New hybrid structures based on memantine and edaravone molecules, in which the pyrazolone ring and adamantane fragments are linked by an alkyl linker, were synthesized. It was found that, in addition to the ability to block the intrachannel site of NMDA receptors, the new hybrid compounds exhibit the property of blockers of the allosteric site of NMDA receptors, which is not inherent in memantine and edaravone preparations. The most active hit compound was determined, which, along with the properties of a two-site blocker of the NMDA receptor, exhibits a pronounced activity as an inhibitor of lipid peroxidation, similarly to the drug edaravone.

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Proteasomes are key components of the ubiquitin-proteasome system. Various forms of proteasomes are known. During aging, disturbances in the functioning of proteasomes have been revealed, as well as increased expression of their particular forms.

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The ubiquitin-proteasome system (UPS) provides hydrolysis of most intracellular proteins in proteasomes. There are various forms of proteasomes that differ, among other things, in the set of proteolytic subunits and the presence of activators. Alzheimer's disease (AD) is characterized by disturbances in the functional state of the UPS.

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A comparative analysis of natural antibodies to β-endorphin, angiotensin, dopamine, serotonin, parameters of the cardiovascular system and anxiety levels was carried out for 241 athletes of various qualifications and sports. The obtained indicators of the cardiovascular system were compared with reference values. A significant increase in the level of natural antibodies to angiotensin was established for all groups of athletes.

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A comparative analysis of specific immunobiochemical parameters, including natural antibodies (NAb) to endogenous regulators of the cardiovascular system, adrenal and gastrointestinal hormones, was performed in students aged 18-22 years with normal and increased body weight (the body mass index from 18.5 to 24.9 kg/m and from 25 to 29.

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Measurement of Immunological Parameters to Assess Human Body Readiness for Physical Load.

Bull Exp Biol Med

December 2021

Department of Biochemical Research, Laboratory of Immunochemistry, Institute of Physiologically Active Substances, Russian Academy of Sciences, Chernogolovka, Moscow Region, Russia.

We measured the level of natural antibodies (nAb) to glutamate and GABA reflecting the balance of excitation and inhibition systems and involved in the adaptation processes in athletes receiving normalized physical activity in the dynamics of training (figure skaters, football players, and people actively involved in sports). It was found that each subject has an individual immunological profile and its parameters change in accordance with the training load. The measured levels of nAbs to GABA and glutamate correlate the physical activity of a person.

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Using the patch-clamp method in the whole cell configuration, it was shown that external potassium ions play an important role in the regulation of calcium-activated chloride channels (CaCCs). A clear dependence of the conductivity of the СаССs on the external potassium concentration was shown. The effect of external potassium in the range 0-15 mM on the conductivity of chloride channels was significantly greater than the effect it had on other ionic currents (sodium or potassium).

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Novel solvent-impregnated resins (SIRs) were prepared by treatment of styrene-divinylbenzene copolymer (LPS-500) with mixtures of the promising polydentante extractant (2-diphenylphosphoryl)-4-ethylphenoxy)methyl)diphenylphosphine oxide (L) and an ionic liquid [Cmim][TfN]for the extraction chromatography recovery of Nd(III) from nitric acid solutions. It was shown that introduction of the ionic liquid into the SIR composition results in considerable enhancement of the Nd(III) recovery efficiency compared with resin impregnated only by L in slightly acidic media. The influence of the L: ionic liquid molar ratio in the SIRs composition, their percentages, concentration of metal and HNO in the eluent, and acid type on the value of synergistic effect and adsorption efficiency of Nd(III) recovery was studied.

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With the aim to find new efficient extractants for recovery of f-block elements from processing wastes of different origin, we have compared a series of phosphoryl-containing podands, including (2-(diphenylphosphorylmethoxy)phenyl)diphenylphosphine oxide and its analogues -, where the ArP(O)Ph group of phosphine oxide type is replaced by phosphonic fragments. Quantum-chemical modelling of the structures of phosphoryl-containing podands and - has been performed, which was later confirmed by the data of X-ray diffraction. The features of extraction of nitric acid, as well as U(VI), Th(IV), Nd(III), and Ho(III) with compounds and - from nitric acid media into 1,2-dichloroethane have been studied.

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Proteasomes are multisubunit complexes that degrade most intracellular proteins. Three of the 14 subunits of the 20S proteasome, specifically β1, β2, and β5, demonstrate catalytic activity and hydrolyze peptide bonds after acidic, basic, and hydrophobic amino acids, respectively. Within proteasome, the constitutive catalytic subunits β1, β2, and β5 can be substituted by the immune βli, β2i, and β5i subunits, respectively.

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[Immunochemical and electromyographic indicators for assessment of pain status in myofascial back pain syndrome].

Zh Nevrol Psikhiatr Im S S Korsakova

January 2021

Russian Medical Academy for Continuous Professional Education, Moscow, Russia.

Objective: A complex examination of patients with chronic myofascial pain syndrome (MPS).

Material And Methods: This study included 136 patients with MPS (66 men and 70 women). Pain was assessed using a Visual Analogue Scale (VAS).

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An unusual greater reactivity of phosphonous propionic acids was found in comparison with phosphonous propionic esters in carbamate version of Kabachnik-Fields reaction. Compounds of tricoordinated phosphorus generated during the amidoalkylation of hydrophosphorylic compounds in acetyl chloride/acetic anhydride mixture were found by P NMR analysis. A hypothesis is proposed about the generation of spirophosphoranes to explain the mechanism for the formation of the phosphorus-carbon bond in the reaction under study.

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Visible to near-IR molecular switches based on photochromic indoline spiropyrans with a conjugated cationic fragment.

Spectrochim Acta A Mol Biomol Spectrosc

April 2020

Institute of Problems of Chemical Physics, Russian Acadeemy of Sciences, 1 Akad. Semenova ave., 142432 Chernogolovka, Moscow Region, Russian Federation.

Photochromic molecules which can absorb and emit light within the "biological window" (650-1450 nm) are of great interest for using in various important biomedical applications such as bio-imaging, photopharmacology, targeted drug delivery, etc. Here we present three new indoline spiropyrans containing conjugated cationic fragments and halogen substituents in the 2H-chromene moiety which were synthesized by a simple one-pot method. The molecular structure of the obtained compounds was confirmed by FT-IR, H and C NMR spectroscopy (including 2D methods), HRMS, elemental and single crystal X-ray analysis.

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Functional and structural features of proteins associated with alternative splicing.

Int J Biol Macromol

March 2020

Department of Bioinformatics, Institute of Biomedical Chemistry, Pogodinskaya street 10, 119121 Moscow, Russia. Electronic address:

The alternative splicing is a mechanism increasing the number of expressed proteins and a variety of these functions. We uncovered the protein domains most frequently lacked or occurred in the splice variants. Proteins presented by several isoforms participate in such processes as transcription regulation, immune response, etc.

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Wave-Like Dose-Dependence of the Stimulating Effects of Dimebon on Cognition in a Wide Dose Range.

Bull Exp Biol Med

October 2019

Laboratory of Biomolecular Screening, Institute of Physiologically Active Substances, Russian Academy of Sciences, Chernogolovka, Moscow region, Russia.

Comparison of the cognition-stimulating effects of Dimebon in a wide dose range revealed a non-monotonic and nontrivial wave-like dose-dependence of its activity. Positive results were obtained at low (0.02-0.

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Ultra-high molecular weight polyethylene (UHMWPE) is a bioinert polymer that is widely used as bulk material in reconstructive surgery for structural replacements of bone and cartilage. Porous UHMWPE can be used for trabecular bone tissue replacement, and it can be used in living cell studies as bioinert 3D substrate permeable to physiological fluids. It is important to develop techniques to govern the morphology of open-cell porous UHMWPE structures (pore size, shape, and connectivity), since this allows control over proliferation and differentiation in living cell populations.

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Imidazoline-based small molecule inhibitors of p53-MDM2 interaction intended for the treatment of p53 wild-type tumors are the promising structures for design of anticancer drugs. Based on fragment approach we have investigated a key role of substituents in cis-imidazoline core for biological activity of nutlin family compounds. Although the necessity of the substituents in the phenyl rings of cis-imidazoline has been shown, there are no studies in which the replacements of a halogen by other substituents have been investigated.

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Antioxidant activity of a pharmaceutical substance hypocard was compared with activity of nitromalic acid and well-known agents nicorandil and Mexidol. The ability of these substances to inhibit spontaneous and oxidant-induced LPO process in rat brain homogenate was analyzed. The mechanisms of these effects were studied.

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Aim: To investigate the ability of the neuroprotector dimebon to prevent alterations in brain lipid metabolism caused byTNF-α.

Material And Methods: The ability of dimebon (2,8-Dimethyl-5-[2-(6-methyl-3-pyridinyl)ethyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole hydrochloride) to prevent alterations in brain lipid metabolism caused byTNF-α was studied in 65 male mice (20+2g weight). TNF-α (10 mkg/mouse), dimebon (0.

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Aim: To evaluate an effect of dimebon on the onset of symptomatic stage in FUS.1-513 transgenic mice - a new genetic model of neurodegeneration, and to study the dynamics of disease progression in the terminal stage.

Material And Methods: The study was carried out on males of line FUS1-513 with the contribution of genes from CD1 strains.

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The levels of natural antibodies to β-endorphin, bradykinin, histamine, dopamine, and serotonin were measured in 271 cardiological patients in order to evaluate the severity of their clinical status. The patients were distributed into groups differing by the course of the pathological process. The levels of natural antibodies to all antigens were maximum in patients with cardiosclerosis: the content of antibodies to β-endorphin surpassed the control by 46%, to histamine by 62%, to bradykinin by 36%, to dopamine by 49%, and to serotonin by 65%.

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Modification of Calcium-Activated Chloride Currents in Cerebellar Purkinje Neurons.

Bull Exp Biol Med

April 2017

Laboratory of Neuroreception, Institute of Physiologically Active Substances, Russian Academy of Sciences, Chernogolovka, Moscow, Region, Russia.

The whole-cell voltage clamp technique was employed to record the total ionic currents in rat cerebellar Purkinje neurons. When intrapipette solution contained 120 mM KCl, replacement of the standard external physiological saline with Na-free solution resulted in appearance of inward tail current after the end of the depolarizing pulse. When intrapipette potassium ions were replaced for cesium ones, the tail currents were observed even in the presence of normal Na concentration (140 mM) in the external solution.

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The evaluation of functional condition of health of sportsmen doing Greek Roman wrestling was implemented using detection of level of antibodies to serotonin, histamine, dopamine, glutamate, GABA, orphanine, endorphin, angiotensin. The study established a reliable increasing of level of antibodies to orphanine, β-endorphin, GABA and glutamate under increasing of duration of physical load. The content of antibodies to other regulators of adaptation had no statistical difference.

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