Advances in Pharmacological and Pharmaceutical Sciences

GABAA Receptor Subtypes: Novel Targets for Novel Medicines


Publishing date
15 Dec 2011
Status
Published
Submission deadline
15 Jun 2011

Lead Editor

1CNS Integration, NeuroSearch A/S, 2750 Ballerup, Denmark

2Janssen Beerse; University of Antwerp, Antwerp, Belgium

3Lilly UK, Erl Manor, Windlesham, Surrey, UK


GABAA Receptor Subtypes: Novel Targets for Novel Medicines

Description

GABAA receptors are located both synaptically and extrasynaptically and are not only important in mediating inhibitory neurotransmission but also represent an important target for medicines used today, including benzodiazepines, the so-called “Z-drug” hypnotics, etomidate, and propofol. Over the last decade, knowledge from various disciplines, notably molecular biology and pharmacology, has propelled our knowledge on GABAA receptors to a point where this knowledge is now being exploited to develop novel medicines. Experiments using exquisite genetically modified mice and pharmacological tool compounds have enhanced our knowledge of the functional roles of different synaptic GABAA receptors and demonstrated that different effects of benzodiazepines, Z-drug hypnotics, and etomidate are mediated via different GABAA receptor subtypes. This has led to the development of novel subtype selective compounds; some of which have been assessed in early stages of clinical development and shown to differ from existing drugs that target GABAA receptors. In addition, extrasynaptic GABAA receptors are not influenced by the majority of clinically available drugs targeting GABAA receptors and therefore represent underexploited targets. However, basic science knowledge on extrasynaptic GABAA receptors and their purported role in insomnia, female stress disorders, major depression, PTSD, and autism suggest these receptors represent fruitful targets for novel medicines.

In this special issue, we would like authors to submit original research or review article that focus on, but are not restricted to, basic research, drug discovery and drug development efforts within the following three GABAA target fields. Potential topics include, but are not limited to:

  • GABAA-α2/α3 selective positive allosteric modulators
  • GABAA-α5 selective positive and negative allosteric modulators
  • δ-containing GABAA receptors

Before submission authors should carefully read over the journal's Author Guidelines, which are located at http://www.hindawi.com/journals/aps/guidelines.html. Prospective authors should submit an electronic copy of their complete manuscript through the journal Manuscript Tracking System at http://mts.hindawi.com/ according to the following timetable:


Articles

  • Special Issue
  • - Volume 2012
  • - Article ID 529861
  • - Editorial

G A B A 𝐀 Receptor Subtypes: Novel Targets for Novel Medicines

Naheed R. Mirza | John Atack | Keith Wafford
  • Special Issue
  • - Volume 2012
  • - Article ID 416864
  • - Review Article

Mechanisms Underlying Tolerance after Long-Term Benzodiazepine Use: A Future for Subtype-Selective G A B A A Receptor Modulators?

Christiaan H. Vinkers | Berend Olivier
  • Special Issue
  • - Volume 2012
  • - Article ID 708428
  • - Review Article

Perisynaptic GABA Receptors: The Overzealous Protector

Andrew N. Clarkson
  • Special Issue
  • - Volume 2012
  • - Article ID 134523
  • - Review Article

An Overview of the CNS-Pharmacodynamic Profiles of Nonselective and Selective GABA Agonists

Xia Chen | Sanne de Haas | ... | Joop van Gerven
  • Special Issue
  • - Volume 2011
  • - Article ID 608912
  • - Research Article

A Comparison of the 𝜶 2/3/5 Selective Positive Allosteric Modulators L-838,417 and TPA023 in Preclinical Models of Inflammatory and Neuropathic Pain

Sarah Nickolls | Hannah Mace | ... | Gordon McMurray
  • Special Issue
  • - Volume 2011
  • - Article ID 578273
  • - Review Article

Central and Peripheral GABAA Receptor Regulation of the Heart Rate Depends on the Conscious State of the Animal

Bo Hjorth Bentzen | Morten Grunnet
  • Special Issue
  • - Volume 2011
  • - Article ID 926361
  • - Review Article

Neurosteroid Binding Sites on the GABAA Receptor Complex as Novel Targets for Therapeutics to Reduce Alcohol Abuse and Dependence

Mary W. Hulin | Russell J. Amato | ... | Peter J. Winsauer
  • Special Issue
  • - Volume 2011
  • - Article ID 153218
  • - Research Article

Chronic Treatment with a Promnesiant GABA-A 𝜶 𝟓 -Selective Inverse Agonist Increases Immediate Early Genes Expression during Memory Processing in Mice and Rectifies Their Expression Levels in a Down Syndrome Mouse Model

J. Braudeau | L. Dauphinot | ... | M. C. Potier
  • Special Issue
  • - Volume 2011
  • - Article ID 790590
  • - Review Article

Augmentation of Tonic GABAA Inhibition in Absence Epilepsy: Therapeutic Value of Inverse Agonists at Extrasynaptic GABAA Receptors

Adam C. Errington | David W. Cope | Vincenzo Crunelli
Advances in Pharmacological and Pharmaceutical Sciences
 Journal metrics
Acceptance rate16%
Submission to final decision93 days
Acceptance to publication32 days
CiteScore4.000
Impact Factor-
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