ReviewInternational journal of medicinal chemistry2015
A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model.
Review in International journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
29 citing papers in PubMed.
- The Role of GABA and Its Receptors in Temporal Lobe Epilepsy.Biomolecules · 2026Review
- Ethanol-induced rapid eye movement sleep suppression in rats: Comparison with subtype-selective GABAJournal of psychopharmacology (Oxford, England) · 2025Article
- New psychoactive substances in roadway crash victims in California.Frontiers in toxicology · 2025Article
- Comparative pharmacodynamic and pharmacokinetic study of MIDD0301 and its (S) enantiomer.Drug development research · 2022Article
- GABAkines - Advances in the discovery, development, and commercialization of positive allosteric modulators of GABAPharmacology & therapeutics · 2022Review
- Development of Inhaled GABAACS pharmacology & translational science · 2022Article
- Prepubescent female rodents have enhanced hippocampal LTP and learning relative to males, reversing in adulthood as inhibition increases.Nature neuroscience · 2022Article
- A multi-dosing regimen to enhance the spatial memory of normal rats with α5-containing GABAPsychopharmacology · 2021Article
- Enantioenriched α-Vinyl 1,4-Benzodiazepines and 1,4-Benzoxazepines via Enantioselective Rhodium-Catalyzed Hydrofunctionalizations of Alkynes and Allenes.The Journal of organic chemistry · 2021Article
- Melanoma Cell Intrinsic GABAInternational journal of radiation oncology, biology, physics · 2021Article
- Herbal Medicinal Products fromTheScientificWorldJournal · 2020Review
- Human Hyperekplexic Mutations in Glycine Receptors Disinhibit the Brainstem by Hijacking GABAiScience · 2019Article
- Modulating native GABAJournal of neuro-oncology · 2019Article
- Novel Benzodiazepine-Like Ligands with Various Anxiolytic, Antidepressant, or Pro-Cognitive Profiles.Molecular neuropsychiatry · 2019Article
- Neurobiology and Therapeutic Potential of α5-GABA Type A Receptors.Frontiers in molecular neuroscience · 2019Article
- Article
- Different Benzodiazepines Bind with Distinct Binding Modes to GABAACS chemical biology · 2018Article
- A Novel Orally Available Asthma Drug Candidate That Reduces Smooth Muscle Constriction and Inflammation by Targeting GABAMolecular pharmaceutics · 2018Article
- GABAergic inhibitory neurons as therapeutic targets for cognitive impairment in schizophrenia.Acta pharmacologica Sinica · 2018Review
- Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ-Aminobutyric Acid Type A Receptor (GABAJournal of medicinal chemistry · 2018Article
Corrections and comments
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Authors and funding
12 authors.
Funding
Abstract
An updated model of the GABA(A) benzodiazepine receptor pharmacophore of the α5-BzR/GABA(A) subtype has been constructed prompted by the synthesis of subtype selective ligands in light of the recent developments in both ligand synthesis, behavioral studies, and molecular modeling studies of the binding site itself. A number of BzR/GABA(A) α5 subtype selective compounds were synthesized, notably α5-subtype selective inverse agonist PWZ-029 (1) which is active in enhancing cognition in both rodents and primates. In addition, a chiral positive allosteric modulator (PAM), SH-053-2'F-R-CH3 (2), has been shown to reverse the deleterious effects in the MAM-model of schizophrenia as well as alleviate constriction in airway smooth muscle. Presented here is an updated model of the pharmacophore for α5β2γ2 Bz/GABA(A) receptors, including a rendering of PWZ-029 docked within the α5-binding pocket showing specific interactions of the molecule with the receptor. Differences in the included volume as compared to α1β2γ2, α2β2γ2, and α3β2γ2 will be illustrated for clarity. These new models enhance the ability to understand structural characteristics of ligands which act as agonists, antagonists, or inverse agonists at the Bz BS of GABA(A) receptors.
Identifiers
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.