Skip to main content Accessibility help

We use cookies to distinguish you from other users and to provide you with a better experience on our websites. Close this message to accept cookies or find out how to manage your cookie settings.

Close cookie message
×
  1. Home
  2. Search

Refine search

Refine search

Access:
Content type:
Publication date:
Apply   From and To filters
Subject: Show more
Journals Show more
Publishers: Show more
Societies Show more
Series: Show more
Collections: Show more

Actions for selected content:

Select all | Deselect all
  • View selected items
  • Export citations
  • Download PDF (zip)
  • Save to Kindle
  • Save to Dropbox
  • Save to Google Drive

Save Search

You can save your searches here and later view and run them again in "My saved searches".

Please provide a title, maximum of 40 characters.
Cancel
×

5 results

  • The original anticonvulsant meta-Cl-benzhydrylurea (m-CL-BHM) induces of the liver monooxygenase system and stimulates the neuroimmune response in behavioral disorders of alcoholic origin

  • Т. Shushpanova, T. Novozheeva, E. Gutkevich, A. Pustovaya, N. Garganeeva, M. Belousov, A. Podyablonsky, E. Markova, E. Knyazeva, O. Shushpanova, N. Kolomiets, S. Safronov, R. Boev
  • Journal:
    European Psychiatry / Volume 65 / Issue S1 / June 2022
    Published online by Cambridge University Press:
    01 September 2022, pp. S819-S820
    • Article
      • You have access
      • Open access
    • PDF
    • Export citation
  • Introduction

    The anticonvulsant m-Cl-BHM is promising for the pathogenetically directed thrapy does not cause negative effects.

    Objectives

    Investigation of the effect of m-Сl-BHM on “immunochemical homeostasis” in rats with experimental alcoholism.

    Methods

    m-Cl-BHM was injected at a dose of 100 mg/kg (1/20 LD50) for 5 and 30 days into the stomach of male Wistar rats who preferred alcohol according to the screening conditions and kept for 10 months. in free access to a 15% ethanol solution, which made up the group of “heavy drinkers” (HD). Phenobarbital was administered at a dose of 25 mg/kg (1/20 LD50).

    Results

    The features of the monooxygenase system of cytochrome P450 of the liver and ECT in the lymphoid organs of rats were studied at different periods of administration of m-CL-BHM -5 and 30 days. to HD rats. m-CL-BHM has an inducing effect on the monooxygenase system of the liver, causes phase changes in the lymphoid organs and ECT. Long-term administration of m-CL-BHM caused a depletion of the cellular composition of lymphoid organs, a decrease in ECT of spleen cells and peritoneal exudate, these changes were less pronounced compared with phenobarbital. The activation of the immune system inversely regulates the production of enzymes of the cytochrome system, since the concentration of low molecular weight targets is sharply reduced with the help of antibodies. m-Cl-BHM metabolites conjugated to endogenous macromolecules form a full-fledged stimulus for the immune system.

    Conclusions

    Neuroimmune response to the introduction of m-CL-BHM is significant in behavioral disorders associated with alcoholism and the correction of this condition.

    Disclosure

    No significant relationships.

  • An innovative anticonvulsant - a GABAA receptor modulator with an alternative mechanism of action and enzyme-inducing detoxifying properties

  • T. Shushpanova, N. Bokhan, K. Stankevich, T. Novozheeva, O. Shushpanova, V. Udut, N. Garganeeva, E. Markova, E. Knyazeva, S. Safronov, R. Boev, A. Solonskii
  • Journal:
    European Psychiatry / Volume 64 / Issue S1 / April 2021
    Published online by Cambridge University Press:
    13 August 2021, pp. S777-S778
    • Article
      • You have access
      • Open access
    • PDF
    • Export citation
  • Introduction

    The development of original drugs - new generation GABAA receptor modulators (GABAAR), with an anti-alcohol orientation, non-addictive and stimulating detoxification processes, makes it possible to increase the effectiveness of therapy and reduce the cost of treatment.

    Objectives

    Study the mechanism of interaction between m-Cl-BHU and GABAA - receptor

    Methods

    Molecular docking was performed to study the molecular docking of m-Cl-BHU with at the binding site of the target protein GABAAR.Radioreceptor studies were carried out using [3H] flunitrazepam binding with synaptosomal receptors in the cerebral cortex of Wistar rats in experimental alcoholism under the influence of therapy with m-CL-BHU. Kinetic parameters (T1/2, Clt, MRT, MET, AUC) of a model substrate - antipyrine were determined in the saliva of healthy volunteers and alcoholic patients.

    Results

    IResults of molecular docking (Schrödinger program (Glide) showed: m-CL-BHU (meta-chlorobenzhydryl urea) is complementary to the benzodiazepine GABAAR. Binding energy is low) (scoring (GScore) -11.14 kKal/mol); m-CL-BHU interacts with key amino acids at the α1γ2 interface: Tyr159, Tyr209, H101 Phe77 and is characterized by a high degree of model fit - dG insert: 0.741 Binding of [3H] flunitrazepam to the benzodiazepine site of GABAAR in rat brain in experimental alcoholism, who received 14 days of m-CL-BHU at 100 mg/kg /day, increased in receptor affinity. Changes in the kinetic parameters (T1/2, Clt, MRT, MET, AUC) of a model substrate - antipyrine in the saliva of healthy volunteers and alcoholic patients using Galodif (m-CL-BHU) at 300 mg/day 21 days

    Conclusions

    m-CL-BHU - GABAA receptor modulator with an alternative mechanism of action

    Disclosure

    No significant relationships.

  • 4 - Methodological issues in psychopharmacogenetics

  • from Part II - Clinical background and research design
    • By Sheldon H. Preskorn, Psychiatric Research Institute, University of Kansas School of Medicine, Wichita, Kansas, USA
  • Edited by Bernard Lerer, Hadassah-Hebrew Medical Center, Jerusalem
  • Book:
    Pharmacogenetics of Psychotropic Drugs
    Published online:
    20 August 2009
    Print publication:
    29 August 2002, pp 57-71

  • Summary

    This chapter discusses methodological issues relevant to conducting pharmacogenetic studies in clinical psychopharmacology. First, basic pharmacologic principles are reviewed, followed by a discussion of the drug development process. In addition to aiding in the drug discovery process, pharmacogenetic finding would also help with the signal:noise problem, at the human testing phase of drug development (that is, phase I through III). Scientists can select the specific subset of the population (that is, those with the genetic variant) likely to respond to the drug. The chapter reviews the significant potential for advancing psychiatric drug development as a result of improved understanding of the pharmacogenetics and pharmacogenomics relevant to the effects of drugs on the human brain. Last, the research linking cytochrome P-450 CPY2D6 poor metabolizers with increased risk of toxicity on routine doses of tricyclic antidepressants (TCAs) are reviewed as an example of the methodological issues encountered when conducting such studies.

  • 8 - Pharmacogenetics of psychotropic drug metabolism

  • from Part IV - Pharmacokinetics
    • By Vural Ozdemir, Centre for Addiction and Mental Health, University of Toronto, Canada; Department of Pharmacology, University of Toronto, Canada, Angela D.M. Kashuba, School of Pharmacy, University of North Carolina, Chapel Hill, USA, Vincenzo S. Basile, Centre for Addiction and Mental Health, University of Toronto, Canada, James L. Kennedy, Centre for Addiction and Mental Health, University of Toronto, Canada
  • Edited by Bernard Lerer, Hadassah-Hebrew Medical Center, Jerusalem
  • Book:
    Pharmacogenetics of Psychotropic Drugs
    Published online:
    20 August 2009
    Print publication:
    29 August 2002, pp 157-180

  • Summary

    Drug metabolism is a critical determinant of therapeutic and adverse effects of many psychotropic drugs. This chapter reviews the basic concepts and definitions pertinent to pharmacogenetics of psychotropic drug metabolism from a clinical psychiatry perspective. It discusses the CYP2D6 genetic polymorphism as a classic example of a monogenic variation in drug metabolism and as a high-affinity and low-capacity elimination route. In addition to genetic contribution to interindividual differences in drug metabolism, the chapter reviews various sources of intraindividual variations and gene-environment interactions of relevance for psychopharmacology. It highlights some of the future research directions in psychotropic drug metabolism and emphasizes the need to evaluate genetic variability in drug metabolism in conjunction with other genes encoding drug transporters, receptors and ion channels, which can all influence individual's risk for adverse drug reactions or therapeutic failure.

  • Measurement of the effect of organic pollution on marine organisms: rapid determination of EROD induction using plate readers

  • Daniel Grzebyk, François Galgani
  • Journal:
    Aquatic Living Resources / Volume 4 / Issue 1 / January 1991
    Published online by Cambridge University Press:
    15 January 1991, pp. 53-59
    Print publication:
    January 1991

  • The purpose of this study was to adapt the ethoxyresorufin O-deethylase (EROD) assay to the microplate technique. In addition to showing the practical advantages related to the intrinsic properties of such systems, we wished to demonstrate their potential value for biological monitoring of contamination in natural environments. A simpliffed procedure was developed for the preparation and fluorimetric assay of EROD activity using only basic laboratory equipment. The use of plate readers allows measurements to be done rapidly and provides numerous advantages in comparison with traditional methods. Within the context of our study; this test could be substituted to advantage for the enzymelinked immunosorbent assay (ELISA).