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Bretazenil binds to both diazepam-sensitive and diazepam-insensitive GABAA receptors . It exhibits powerful anxiolytic and anticonvulsant properties . In animal models, bretazenil has been shown to be approximately 60 times more potent than midazolam in blocking the pentylenetetrazole cue .
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Research chemicals are specialized synthetic substances created exclusively for scientific and laboratory investigations. These compounds are not approved for human consumption or therapeutic use; they are solely intended for usage in controlled laboratory environments. Research chemicals may include novel compounds, analogs of existing drugs, or substances specifically designed to study biological processes and molecular interactions.
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Drug Discovery:Â Research chemicals play a key role in generating lead compounds and evaluating their potential in preclinical studies, including high-throughput screening, hit-to-lead optimization, and structure-activity relationship (SAR) studies.
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Understanding Bretazenil Scientific Background
Chemical Identity and Properties
Bretazenil is an imidazobenzodiazepine with the IUPAC name (13aS)-8-bromo-11,12,13,13a-tetrahydro-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylic acid 1,1-dimethylethyl ester . The compound has a CAS number 84379-13-5 .
Key Physical Properties:
Molecular Formula:Â C19H20BrN3O3Â
Molecular Weight:Â 418.28 g/molÂ
Appearance:Â White to off-white crystalline solidÂ
Purity: ≥98% (HPLC)Â
Solubility: Soluble to 100 mM in DMSO and ethanol ; <41.83mg/ml in ethanol and DMSOÂ
Storage: Store at -20°C; desiccate at +4°CÂ
CAS Number:Â 84379-13-5Â
EC50: 10 nM at α1β1γ2 receptorsÂ
Receptor Pharmacology
Bretazenil acts as a partial agonist at the GABAA benzodiazepine site . It binds to GABAA receptors that are both sensitive and insensitive to diazepam .
Key pharmacological findings include:
Parameter Value EC50 (α1β1γ2) 10 nM Potency vs. Midazolam ~60x more potent in PTZ-cue antagonism Potency vs. Diazepam ~10x more potent Efficacy at GABAA 25-50% of full agonists Stereoisomer Activity S-isomer >1000x more potent than R-isomer Pharmacological Profile
Bretazenil produces anticonvulsant and anxiolytic effects with lower efficacy for motor impairment and sedation in preclinical models :
Anticonvulsant:Â Potent in audiogenic and pentylenetetrazol-induced seizure modelsÂ
Anxiolytic:Â Effective in conflict tests and elevated plus mazeÂ
Attenuated Side Effects:Â Virtually fails to induce motor impairment or severe sedation in animal modelsÂ
Pharmacokinetics and Metabolism
Bretazenil possesses a half-life of approximately 2 to 4.5 hours and is quickly absorbed . A recent comprehensive metabolism study identified a total of 26 metabolites using in vitro and in vivo samples :
Predominant Pathway:Â Hydroxylation on the pyrrolidine ringÂ
Phase II Reactions:Â O-glucuronidation, sulfation, and methylationÂ
Key Metabolites:Â Hydroxy-bretazenil (B14), reduced hydroxy-bretazenil (B6), and reduced dihydroxy-bretazenil (B1) are recommended as significant markers for detecting bretazenil useÂ
Research Applications
Receptor Pharmacology: The molecular mechanisms of bretazenil’s partial agonism have been studied in native and recombinant GABAA receptors . In cortical neurons, bretazenil’s efficacy was lower than diazepam with similar potency .
Behavioral Pharmacology: Preclinical studies have evaluated bretazenil’s effects on punished responding and drug discrimination . Antagonists such as flumazenil and ZK 93,426 have been used to block bretazenil’s behavioral effects .
Forensic and Analytical Chemistry:Â Bretazenil and its metabolites can be detected and quantified in biological matrices using LC-MS/MS and UHPLC-HRMS/MSÂ .
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When you buy Bretazenil online, understanding the importance of product quality is essential for successful research outcomes. Research is only as reliable as the compounds you use. Bretazenil is a synthetic compound with a defined stereocenter at position 13a . The S-isomer is significantly more potent than the R-isomer , making enantiomeric purity critical for research results.
Key Quality Indicators:
Purity: Our ≥98% purity ensures minimal interference in research protocolsÂ
Enantiomeric Purity:Â Consistent stereochemistry for accurate researchÂ
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Storage:Â Proper handling and storage conditions maintained throughout distribution
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Bretazenil is a synthetic compound with a defined stereocenter . The presence of impurities or incorrect isomers can compromise research results. Our lab-tested Bretazenil is verified to ≥98% purity, ensuring accurate and reproducible experimental outcomes .2. Regulatory Compliance
Bretazenil has emerged on the illicit drug market as a new designer benzodiazepine . It is monitored by organizations such as the UNODC and EUDA Early Warning Systems . Purchasing from a legitimate supplier ensures compliance with applicable regulations.3. Forensic and Research Legitimacy
For forensic and analytical research, traceability and documentation are essential. Our Bretazenil is supplied with Certificates of Analysis confirming identity and purity, meeting the requirements of analytical laboratories.4. Safety Considerations
Bretazenil has been associated with significant sedative effects in clinical studies. Phase I studies demonstrated that bretazenil induced substantial decrements in attention, numerical memory, psychomotor activity, wakefulness, and critical flicker fusion frequency . At doses of 0.5 mg, most subjects were sedated to the point that they could not adequately perform eye tracking and movement tests . These findings underscore the importance of handling Bretazenil only in controlled laboratory settings with appropriate safety protocols. Explore Our Bretazenil Selection
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Product Specifications
Chemical Name:Â (13aS)-8-Bromo-11,12,13,13a-tetrahydro-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylic acid 1,1-dimethylethyl ester / Ro 16-6028Â
CAS Number:Â 84379-13-5Â
Molecular Formula:Â C19H20BrN3O3Â
Molecular Weight:Â 418.28 g/molÂ
Appearance:Â White to off-white crystalline solidÂ
Purity: ≥98% (HPLC)Â
EC50 (α1β1γ2): 10 nMÂ
Solubility:Â Soluble to 100 mM in DMSO and ethanolÂ
Storage: Store at -20°C ; desiccate at +4°CÂ
Shipping:Â Room temperature in continental US
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General Storage Guidelines:
Containers
Chemicals must be stored in containers made of material compatible with the chemical
Containers must be in good condition with no signs of cracks or corrosion
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Ensure all containers are clearly labeled with the chemical’s full name, CAS number, owner’s name, date of receipt, and any necessary hazard information
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Store oxidizers away from organics and reducing agents
Store organics and inorganics separately
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For compounds like Bretazenil, storage at -20°C with protection from light is recommendedÂ
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Recommended Storage Conditions for Bretazenil:
Parameter Recommendation Storage Temperature -20°C ; desiccate at +4°C Light Protection Yes Container Well-closed, airtight Solution Stability Store at -20°C, use within 1 month; aliquot to avoid freeze/thaw cycles Lyophilized Stability Stable for 36 months at -20°C Best Practices:
Store chemicals on sturdy, level shelving with liquid chemicals not stored above eye level
Do not store chemicals on the floor unless in secondary containment
Return chemicals to their designated storage promptly after use
Schedule regular inventories and remove expired chemicals
If incompatible materials must be stored in the same cabinet, provide secondary containment and segregation
Use desiccators for chemicals that react with air or water or are hygroscopic
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 Frequently Asked Questions (FAQs)
Q: What is Bretazenil (Ro 16-6028)?
A: Bretazenil is a highly potent benzodiazepine that acts as a partial agonist at the GABAA receptor . It was developed in the 1980s but never marketed as a medicine .Q: What is the CAS number for Bretazenil?
A: The CAS number for Bretazenil is 84379-13-5Â .Q: What is the purity of your Bretazenil?
A: Our Bretazenil is lab-tested and meets rigorous quality standards with ≥98% purity . Certificate of analysis is available upon request.Q: How should I store Bretazenil?
A: Store in a well-closed container at -20°C . For lyophilized form, stability is 36 months at -20°C. For solutions, store at -20°C and use within 1 month to prevent loss of potency .Q: What are the physical properties of Bretazenil?
A: Bretazenil has a molecular formula of C19H20BrN3O3 and a molecular weight of 418.28 g/mol . It appears as a white to off-white crystalline solid .Q: What is the mechanism of action of Bretazenil?
A: Bretazenil acts as a partial agonist at the GABAA benzodiazepine site, with an EC50 of 10 nM at α1β1γ2 receptors . It binds to both diazepam-sensitive and diazepam-insensitive GABAA receptors .Q: What are the research applications of Bretazenil?
A: Bretazenil is used in GABAA receptor pharmacology studies, comparative research on partial versus full agonists, analytical method development, and forensic and toxicological research for NPS detection .Q: What payment methods do you accept?
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A: Yes, overnight shipping is available for qualifying orders. Buy Bretazenil with fast shipping and receive your order quickly.Q: What is the legal status of Bretazenil?
A: Bretazenil has emerged on the illicit drug market as a new designer benzodiazepine and is monitored by the UNODC and EUDA Early Warning Systems . It is intended for research purposes only. Please ensure compliance with all applicable laws in your jurisdiction.Q: What are the metabolites of Bretazenil?
A: A total of 26 metabolites have been identified . The predominant pathway involves hydroxylation on the pyrrolidine ring . Key metabolites include hydroxy-bretazenil (B14), reduced hydroxy-bretazenil (B6), and reduced dihydroxy-bretazenil (B1) .Q: Is a Certificate of Analysis (COA) provided with my order?
A: Yes, every order comes with a Certificate of Analysis confirming the identity and purity of the product.Q: Can I use Bretazenil for human consumption?
A: No. This product is intended for research and laboratory applications only. It is not for human or veterinary use.Q: What is the half-life of Bretazenil?
A: Bretazenil has a half-life of approximately 2 to 4.5 hours and is quickly absorbed .Q: Is Bretazenil a full or partial agonist?
A: Bretazenil is a partial agonist at the GABAA benzodiazepine site . Its efficacy is lower than that of full agonists like diazepam .Q: What analytical methods are used to detect Bretazenil?
A: LC-MS/MS, GC-MS, and UHPLC-HRMS/MS are commonly used for the detection and quantification of Bretazenil in biological matrices ÂLegal Disclaimer: This product is intended for research and laboratory applications only. It is not for human or veterinary use. Bretazenil is monitored by the UNODC and EUDA Early Warning Systems as a new designer benzodiazepine . This product is intended for research and forensic purposes only. Must be 21+ to purchase. Ensure compliance with all applicable laws and regulations in your jurisdiction
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