Desalkylgidazepam
Desalkylgidazepam (Bromonordiazepam) is the major active metabolite of Gidazepam (HY-U00315) and a benzodiazepine agent. Desalkylgidazepam activates GABAA receptors, binds to the benzodiazepine site, enhances GABA-mediated inhibitory neurotransmission, and potentiates GABA-induced chloride ion influx through positive allosteric modulation at α1β2γ2 receptors.
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- CAS. Nr.: 2894-61-3
- Formel: C15H11BrN2O
- Molecular Weight:315.16
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
13.9 nM
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Desalkylgidazepam EC50 for positive allosteric modulation of 2 μM GABA-induced currents in CHO cells expressing human α1β2γ2 GABAA receptors by automated whole-cell patch-clamp electrophysiology.
Desalkylgidazepam EC50 for positive allosteric modulation of 2 μM GABA-induced currents in CHO cells expressing human α1β2γ2 GABAA receptors by automated whole-cell patch-clamp electrophysiology.
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41946818 |
In Vitro
Desalkylgidazepam (0.96-3000 nM) acts as a positive allosteric modulator at α1β2γ2 GABAA receptors expressed in CHO cells, with an EC50 of 13.9 nM, and its enhancement effect can be abolished by Flumazenil (HY-B0009)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2894-61-3
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Molecular Weight 315.16
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Formel C15H11BrN2O
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SMILES
O=C1NC2=C(C(C3=CC=CC=C3)=NC1)C=C(Br)C=C2
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Synonyms
Bromonordiazepam
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[2]. Manchester KR, et al. The blood-to-plasma ratio and predicted GABA-binding affinity of designer benzodiazepines. Forensic toxicology. 2022 Jul;40(2):349-356. [Content Brief]
[3]. Mérette SAM, et al. Desalkylgidazepam blood concentrations in 63 forensic investigation cases. Journal of analytical toxicology. 2023 Dec 12;47(9):858-866. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Desalkylgidazepam Related Classifications
HY-W634748 Related Classifications
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Keywords
- Desalkylgidazepam
- 2894-61-3
- Bromonordiazepam
- GABA Receptor
- Drug Metabolite
- Chloride Channel
- GABA-mediated inhibitory neurotransmission
- GABAA receptors
- benzodiazepine
- benzodiazepine site
- chloride ion flux
- human hepatocytes
- hydroxylation
- positive allosteric modulation
- translocator protein TSPO
- α1β2γ2 receptors
- Inhibitor
- inhibitor
- inhibit