ArticleBritish journal of pharmacology2019
A photoswitchable GABA receptor channel blocker.
Article in British journal of pharmacology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Preparation, characterization and application of MT@SP@GBP and their use for synthesis of novel pyrazolophthalazine-5,10-diones.Scientific reports · 2025Article
- Integrating single-cell sequencing and machine learning to uncover the role of mitophagy in subtyping and prognosis of esophageal cancer.Apoptosis : an international journal on programmed cell death · 2025Article
- Light-Activated Agonist-Potentiator of GABAJournal of the American Chemical Society · 2024Article
- VHH Nanobody Versatility against Pentameric Ligand-Gated Ion Channels.Journal of medicinal chemistry · 2024Review
- Light-Based Anti-Biofilm and Antibacterial Strategies.Pharmaceutics · 2023Review
- Action of the Photochrome Glyght on GABAergic Synaptic Transmission in Mouse Brain Slices.International journal of molecular sciences · 2022Article
- Enlightening the "Spirit Molecule": Photomodulation of the 5-HTAngewandte Chemie (International ed. in English) · 2022Article
- Review
- Electroacupuncture Suppresses CCI-Induced Neuropathic Pain through GABAA Receptors.Evidence-based complementary and alternative medicine : eCAM · 2022Article
- Photopharmacology of Ion Channels through the Light of the Computational Microscope.International journal of molecular sciences · 2021Review
- Optical Control of GABAChemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
- Photopotentiation of the GABAProceedings of the National Academy of Sciences of the United States of America · 2019Article
- A photoswitchable GABA receptor channel blocker.British journal of pharmacology · 2019Article
- Article
Corrections and comments
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Authors and funding
14 authors.
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No grant is acknowledged in the PubMed record.
Abstract
background and purposeAnion-selective Cys-loop receptors (GABA and glycine receptors) provide the main inhibitory drive in the CNS. Both types of receptor operate via chloride-selective ion channels, though with different kinetics, pharmacological profiles, and localization. Disequilibrium in their function leads to a variety of disorders, which are often treated with allosteric modulators. The few available GABA and glycine receptor channel blockers effectively suppress inhibitory currents in neurons, but their systemic administration is highly toxic. With the aim of developing an efficient light-controllable modulator of GABA receptors, we constructed azobenzene-nitrazepam (Azo-NZ1), which is composed of a nitrazepam moiety merged to an azobenzene photoisomerizable group. EXPERIMENTAL APPROACH: The experiments were carried out on cultured cells expressing Cys-loop receptors of known subunit composition and in brain slices using patch-clamp. Site-directed mutagenesis and molecular modelling approaches were applied to evaluate the mechanism of action of Azo-NZ1. KEY
resultsAt visible light, being in trans-configuration, Azo-NZ1 blocked heteromeric α1/β2/γ2 GABA CONCLUSIONS AND IMPLICATIONS: Azo-NZ1 is a soluble light-driven Cl-channel blocker, which allows photo-modulation of the activity induced by anion-selective Cys-loop receptors. Azo-NZ1 is able to control GABAergic postsynaptic currents and provides new opportunities to study inhibitory neurotransmission using patterned illumination.
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