Abstract
A successful unified pharmacophore/receptor model which has guided the synthesis of subtype selective compounds is reviewed in light of recent developments both in ligand synthesis and structural studies of the binding site itself. The evaluation of experimental data in combination with a comparative model of the α1β2γ2 GABAA receptor leads to an orientation of the pharmacophore model within the Bz BS. Results not only are important for the rational design of selective ligands, but also for the identification and evaluation of possible roles which specific residues may have within the benzodiazepine binding pocket.
Keywords: Aminobutyric acid(A) receptors, gated ion channels, GABA-A, computer-assisted analysis, benzodiazepine
Current Medicinal Chemistry
Title: An Updated Unified Pharmacophore Model of the Benzodiazepine Binding Site on γ-Aminobutyric Acida Receptors: Correlation with Comparative Models
Volume: 14 Issue: 26
Author(s): T. Clayton, J. L. Chen, M. Ernst, L. Richter, B. A. Cromer, C. J. Morton, H. Ng, C. C. Kaczorowski, F. J. Helmstetter, R. Furtmuller, G. Ecker, M. W. Parker, W. Sieghart and J. M. Cook
Affiliation:
Keywords: Aminobutyric acid(A) receptors, gated ion channels, GABA-A, computer-assisted analysis, benzodiazepine
Abstract: A successful unified pharmacophore/receptor model which has guided the synthesis of subtype selective compounds is reviewed in light of recent developments both in ligand synthesis and structural studies of the binding site itself. The evaluation of experimental data in combination with a comparative model of the α1β2γ2 GABAA receptor leads to an orientation of the pharmacophore model within the Bz BS. Results not only are important for the rational design of selective ligands, but also for the identification and evaluation of possible roles which specific residues may have within the benzodiazepine binding pocket.
Export Options
About this article
Cite this article as:
Clayton T., Chen L. J., Ernst M., Richter L., Cromer A. B., Morton J. C., Ng H., Kaczorowski C. C., Helmstetter J. F., Furtmuller R., Ecker G., Parker W. M., Sieghart W. and Cook M. J., An Updated Unified Pharmacophore Model of the Benzodiazepine Binding Site on γ-Aminobutyric Acida Receptors: Correlation with Comparative Models, Current Medicinal Chemistry 2007; 14(26) . https://dx.doi.org/10.2174/092986707782360097
DOI https://dx.doi.org/10.2174/092986707782360097 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |

- Author Guidelines
- Editorial Policies
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Allegations from Whistleblowers
- Publishing Ethics and Rectitude
- Increase Visibility Of Your Article
- Archiving Policies
- Reviewer Guidelines
- Guest Editor Guidelines
- Board Recruitment Workflow
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Announcements
- Forthcoming Thematic Issues
Related Articles
-
Selective Modulators of α<sub>5</sub>-Containing GABA<sub>A</sub> Receptors and their Therapeutic Significance
Current Drug Targets Role of Gap Junction Channel in the Development of Beat-to-Beat Action Potential Repolarization Variability and Arrhythmias
Current Pharmaceutical Design Ionotropic Glutamate Receptor Biology: Effect on Synaptic Connectivity and Function in Neurological Disease
Current Medicinal Chemistry Clinical Applications of Positron Emission Tomography (PET) Imaging in Medicine: Oncology, Brain Diseases and Cardiology
Current Radiopharmaceuticals Latest Advances Towards the Discovery of 5-HT7 Receptor Ligands
Mini-Reviews in Medicinal Chemistry Anticonvulsant, Anxiolytic and Antidepressant Properties of the β-caryophyllene in Swiss Mice: Involvement of Benzodiazepine-GABAAergic, Serotonergic and Nitrergic Systems
Current Molecular Pharmacology Longitudinal Melatonin Production in Female Laboratory Rats During 1997-2006: Possible Modulatory Effects of Changing Solar Activity
Current Aging Science Editorial [Is Drug Safety Dangerous?]
Current Drug Safety Potential Therapeutic Targets for Neurodegenerative Diseases: Lessons Learned from Calorie Restriction
Current Drug Targets Competitive Gly/NMDA Receptor Antagonists
Current Topics in Medicinal Chemistry Editorial (Thematic Issue: Global Trends for Nanotechnological Approaches in Various Health Issues - Part 1)
Current Drug Metabolism Synthesis and Pharmacological Screening of Novel 1,3-Disubstituted 5-Pyrazolones as Anticonvulsant Agents
Current Bioactive Compounds Neuroprotection for Amyotrophic Lateral Sclerosis: Role of Stem Cells, Growth Factors, and Gene Therapy
Central Nervous System Agents in Medicinal Chemistry Role of Nitric Oxide and Calpain Activation in Neuronal Death and Survival
Current Drug Targets - CNS & Neurological Disorders Co-Enzyme Q10 to Treat Neurological Disorders: Basic Mechanisms, Clinical Outcomes, and Future Research Direction
CNS & Neurological Disorders - Drug Targets Patent Annotations
Recent Patents on CNS Drug Discovery (Discontinued) Editorial (Thematic Issue: Polypharmacology in Drug Discovery)
Current Pharmaceutical Design Adenosine and Related Drugs in Brain Diseases: Present and Future in Clinical Trials
Current Topics in Medicinal Chemistry Synthesis, Neurotoxicity and Anticonvulsant Study of Some Benzothiazole Analogs
Letters in Drug Design & Discovery Voltage-Dependent Na+ Channels as Targets of BACE1 - Implications for Neuronal Firing and Beyond
Current Alzheimer Research