New non-opioid analgesics : understanding molecular mechanisms on the basis of patch-clamp and quantum-chemical studies / authored by Boris V. Krylov [and four others].

Format:

Book

Author/Creator:

Krylov, Boris V, Author.

Krylov, Boris V., author.

Series:

Frontiers in Pain Science, 2542-9175 ; Volume 1

Language:

English

Subjects (All):

Opioids--Receptors.

Opioids.

Physical Description:

1 online resource (204 pages) : illustrations.

Edition:

1st ed.

Place of Publication:

Sharjah, United Arab Emirates : Bentham Science Publishers, 2017.

Summary:

The monograph is a summary of methods used to study pain receptors and the results obtained in some experiments designed to study the effect of non-opioid analgesics. The molecular mechanisms of nociceptive information control in primary sensory nociceptive neurons are described based on investigations of the membrane signaling cascade (opioid-like receptor - Na+ K+-ATPase - NaV1.8 channel) observed by the authors. Based on this data the authors conclude that the modulation of NaV1.8 channels responsible for the coding of noxious signals can be carried out due to two novel targeting mechanisms. The first of these is the activation of opioid-like receptors; the second is the activation of Na+/K+-ATPase as a signal transducer. The development of a novel class of analgesics that trigger these mechanisms should lead to a successful solution to the problem of chronic pain relief. Chapters of the monograph cover the general methods used in studying nociceptive pain (including the patch-clamp method) and the mechanism behind the binding of different ligands to these receptors such gamma-pyrones gamma-pyridines and cardiotonic steroids. This monograph is a valuable reference for neuroscientists pharmacologists and allied researchers studying pain receptors for the development of safe and effective analgesics.

Contents:

Intro

CONTENTS

PREFACE

Introduction and Methodology

PHYSIOLOGY OF PRIMARY SENSORY CODING

ROLE OF ION CHANNELS IN PRIMARY SENSORY CODING

Selectivity Filter

Inactivation Gating Device

Activation Gating Device

LIMITING SLOPE PROCEDURE

Mathematical Modeling of Zeff Evaluation by the Limiting Logarithmic Voltage Sensitivity Method

m-model

m3-model

m3h_s-model

m3h_f-model

PROBABLE ROLE OF EFFECTIVE CHARGE TRANSFER IN NOCICEPTIVE INFORMATION CODING

PATCH-CLAMP RESULTS OF ZEFF EVALUATION BY THE LIMITING LOGARITHMIC VOLTAGE SENSITIVITY METHOD

CONCLUSION

CONFLICT OF INTEREST

ACKNOWLEDGEMENTS

REFERENCES

Possible Mechanisms of Binding of Gamma-Pyrones to the Opioid-Like Receptor

PATCH-CLAMP INVESTIGATION OF GAMMA-PYRONES

QUANTUM-CHEMICAL STUDY OF GAMMA-PYRONES

Free Acids

Acid Anions

Sodium and Calcium Salts

Complexes with Ca2+

Sodium and Calcium Salts of Ca2+ Complexes

Energy Effects of Salt Formation and Ca2+ Chelation

Possible Mechanisms of Binding of Gamma-Pyridones to the Opioid-Like Receptor

PATCH-CLAMP INVESTIGATION OF GAMMA-PYRIDONES

QUANTUM-CHEMICAL STUDY OF GAMMA-PYRIDONES

Calcium Salts

Сalcium Salts of Ca2+ Complexes

Structure of Molecule F (5-hydroxy-2-hydroxymethyl-gamma-pyridone)

Possible Mechanisms of Ligand-Receptor Binding of Cardiotonic Steroids

PATCH-CLAMP INVESTIGATION OF CARDIOTONIC STEROIDS

QUANTUM-CHEMICAL STUDY OF CARDIOTONIC STEROIDS

Ouabain and Ouabagenin

Ouabain-Ca2+ Chelate Complexes

Ouabagenin-Ca2+ Chelate Complexes

Marinobufagenin

CONCLUSION.

CONFLICT OF INTEREST

Concluding Remarks

OPIOID-LIKE RECEPTOR-COUPLED MECHANISM OF NAV1.8 CHANNELS MODULATION

TRANSDUCER-COUPLED MECHANISM OF NAV1.8 CHANNELS MODULATION

MODULATED RECEPTOR MECHANISM OF NAV1.8 CHANNELS CONTROL

GLOSSARY

SUBJECT INDEX.

Notes:

Includes bibliographical references at the end of each chapters and index.

Description based on online resource; title from PDF title page (ebrary, viewed August 10, 2017).

ISBN:

9781608059300

1608059308

OCLC:

994713552