Diversity and Functions of GABA Receptors: A Tribute to Hanns Möhler, Part A - 1st Edition - ISBN: 9780128026601, 9780128026922

Diversity and Functions of GABA Receptors: A Tribute to Hanns Möhler, Part A, Volume 72

1st Edition

Serial Volume Editors: Uwe Rudolph
eBook ISBN: 9780128026922
Hardcover ISBN: 9780128026601
Imprint: Academic Press
Published Date: 12th January 2015
Page Count: 282
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Table of Contents

  • Preface: A Tribute to Professor Hanns Möhler
  • Chapter One: The Legacy of the Benzodiazepine Receptor: From Flumazenil to Enhancing Cognition in Down Syndrome and Social Interaction in Autism
    • Abstract
    • 1 Introduction
    • 2 Discovery of the Benzodiazepine Receptor
    • 3 Dr. Ziegler, a First for Flumazenil
    • 4 Where are the Selective Anxiolytics?
    • 5 Role of α2 GABAA Receptors in Circuits of Risk Assessment and Fear
    • 6 Comorbidity of Anxiety States and Depression: A Telling Animal Model
    • 7 Powerful, Nonsedative GABAergic Analgesics
    • 8 Cognitive Behavior Targeted via α5 GABAA Receptors
    • 9 Down Syndrome: Start of a Clinical Trial Targeting Cognitive Dysfunction
    • 10 Autism Spectrum Disorders: Beneficial Benzodiazepine Actions at Very Low Dose
    • 11 Conclusion
    • Conflict of Interest
  • Chapter Two: Behavioral Functions of GABAA Receptor Subtypes - The Zurich Experience
    • Abstract
    • 1 Introduction: GABAA Receptor Research at the Institute of Pharmacology and Toxicology of the University of Zurich
    • 2 Behavioral Functions of the γ2 Subunit
    • 3 Genetic Dissection of the Pharmacological Functions of GABAA Receptors Using α Subunit Knock-in Mice
    • 4 Switching Efficacy from Negative to Positive Allosteric Modulation by Histidine to Arginine Point Mutations
    • 5 Interaction of Benzodiazepines and Ethanol
    • 6 Role of β3-Containing GABAA Receptors in the Action of General Anesthetics
    • 7 Role of α5-Containing GABAA Receptors in the Development of Tolerance
    • 8 Glutamatergic Forebrain Neurons Mediate the Sedative Action of Diazepam
    • 9 Memory for Location and Objects Requires α5-Containing GABAA Receptors
    • 10 Diazepam-Induced Changes in Respiration: Role of α1- and α2-Containing GABAA Receptors
    • 11 Modulation of Defensive Behavioral Reactivity to Mild Threat
    • 12 Conclusion
    • Conflict of Interest
    • Acknowledgments
  • Chapter Three: Allosteric Modulation of GABAA Receptors via Multiple Drug-Binding Sites
    • Abstract
    • 1 Introduction
    • 2 Structure of GABAA Receptors
    • 3 GABA-Binding Sites
    • 4 Benzodiazepine-Binding Sites
    • 5 Picrotoxinin-Binding Sites
    • 6 Binding Sites for Anesthetics
    • 7 Alcohol-Binding Sites
    • 8 Cannabinoid-Binding Site
    • 9 Avermectin B1a-Binding Site
    • 10 Binding Sites of Ions
    • 11 Conclusion
    • Conflict of Interest
  • Chapter Four: Regulation of GABAARs by Phosphorylation
    • Abstract
    • 1 Introduction
    • 2 The γ-Aminobutyric Acid Type a Receptors
    • 3 Phosphorylation Sites on GABAAR
    • 4 GABAAR-Interacting Proteins and Phosphorylation
    • 5 Phosphorylation and Allosteric Modulation
    • 6 Signaling Pathways that Modulate GABAAR Phosphorylation
    • 7 Dysregulation of GABAAR Phosphorylation in Disease
    • 8 Conclusion
  • Chapter Five: Endozepines
    • Abstract
    • 1 Introduction
    • 2 Physiological Evidence of Endozepines
    • 3 Candidate Endozepines
    • 4 Diazepam-Binding Inhibitor
    • 5 Conclusion
    • Conflict of Interest
  • Chapter Six: Inhibitory Neurosteroids and the GABAA Receptor
    • Abstract
    • 1 Introduction
    • 2 Structure–Function of Inhibitory Neurosteroids
    • 3 Physiological Effects of Inhibitory Neurosteroids at GABAARs
    • 4 Potential Inhibitory Neurosteroid-Binding Sites on GABAARs
    • 5 The Potentiating Neurosteroid-Binding Site Is Unaffected by Inhibitory Neurosteroids
    • 6 Inhibitory Neurosteroid-Binding Site Outside the Ion Channel—C. elegans and UNC-49
    • 7 Conclusion
    • Conflict of Interest
    • Acknowledgment
  • Chapter Seven: Interactions of Flavonoids with Ionotropic GABA Receptors
    • Abstract
    • 1 Introduction
    • 2 6-Substituted Flavones
    • 3 Flavan-3-ol Esters
    • 4 (+)-Catechin and α4βδ GABAA Receptors
    • 5 Natural Flavonoids and Related Compounds
    • 6 Conclusion
    • Conflict of Interest
    • Acknowledgments
  • Chapter Eight: GABAA Receptor Partial Agonists and Antagonists: Structure, Binding Mode, and Pharmacology
    • Abstract
    • 1 Introduction
    • 2 GABAAR Antagonists
    • 3 GABAAR Partial Agonists
    • 4 Pharmacological Applications of GABAA Antagonists
    • 5 Conclusion
    • Conflict of Interest
    • Acknowledgments
  • Chapter Nine: Closing the Gap Between the Molecular and Systemic Actions of Anesthetic Agents
    • Abstract
    • 1 Introduction
    • 2 Classical Theories of General Anesthesia
    • 3 Point Mutations in GABAA Receptors Affecting Anesthetic Potency
    • 4 Neuroanatomical Substrates for General Anesthetics
    • 5 Homeostatic Regulations in Knockout Animals
    • 6 Anesthetic-Resistant Mice
    • 7 The Hypnotic Action of Etomidate
    • 8 Etomidate-Induced Hypnosis and Subtype-Specific Electroencephalogram Signatures
    • 9 Benzodiazepine-Induced Sedation Does Not Manifest in the EEG
    • 10 Different Roles of α2- and α3-Subunits in Modulating Brain Electrical Activity
    • 11 Intracortical Actions of Etomidate
    • 12 Actions of Etomidate in the Hippocampus
    • 13 Spinal Actions of Etomidate
    • 14 Anesthetic Side Effects
    • 15 Multisite and Multiple Molecular Actions of General Anesthetics
    • 16 Agent-Specific Actions of Anesthetics Lacking Binding Selectivity
    • 17 Conclusion
    • Conflict of Interest
    • Acknowledgments
  • Index


This new volume of Advances in Pharmacology presents the diversity and functions of GABA Receptors. The volume looks at research performed in the past 20 years which has revealed specific physiological and pharmacological functions of individual GABAA receptor subtypes, providing novel opportunities for drug development.

Key Features

  • Contributions from the best authors in the field
  • An essential resource for pharmacologists, immunologists, and biochemists


Pharmacologists and Neuroscientists


No. of pages:
© Academic Press 2015
Academic Press
eBook ISBN:
Hardcover ISBN:


Praise for the Series:
"...recommended not only to pharmacologists but also to all those in related disciplines" --Nature

Ratings and Reviews

About the Serial Volume Editors

Uwe Rudolph

Uwe Rudolph Serial Volume Editor

Dr. Rudolph is Director of the Laboratory of Genetic Neuropharmacoloy at McLean Hospital and Professor of Psychiatry at Harvard Medical School. He studied medicine and completed a research thesis on G proteins at the Freie Universitat Berlin, Germany. After postdoctoral training at Baylor College of Medicine in Houston, Texas, where he developed a mouse model of inflammatory bowel disease and colon cancer, he moved to the Institute of Pharmacology and Toxicology of the University of Zurich to work on GABAA receptors. There, he developed different lines of knock-in mice in which diazepam-sensitive GABAA receptor subtypes were rendered insensitive to diazepam by a histidine to arginine point mutation. Studying these mice enables researchers to uncover unique functional roles of GABAA receptor subtypes. In 2005, he joined McLean Hospital in Belmont, MA, and Harvard Medical School, where his research group is elucidating the functions of GABAA receptor subtypes in defined neuronal populations.

Affiliations and Expertise

Genetic Neuropharmacology Laboratory, McLean Hospital, Belmont, MA, USA