Flubrotizolam (2-bromo-4-(2-fluorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine) is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects, which has been sold as a designer drug.
Flubrotizolam
Cat. No. B3025693
CAS RN: 57801-95-3
M. Wt: 377.2 g/mol
InChI Key: VOZDBDBHBXLWCG-UHFFFAOYSA-N
Attention: For research use only. Not for human or veterinary use.
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- Click on QUICK INQUIRY to receive a quote from our team of experts.
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Description
Flubrotizolam is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects . It has been sold as a designer drug . The IUPAC name for Flubrotizolam is 4-bromo-7-(2-fluorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.0 2,6]trideca-2(6),4,7,10,12-pentaene .
Molecular Structure Analysis
Flubrotizolam has a complex molecular structure. It is composed of a benzene ring fused to a seven-triazole membered 1,4-diazepine ring that is also fused to a 1,2,4 ring . An alkyl methyl (-CH3) is attached at the 1-position of the triazole ring, a 2-fluorophenyl ring is attached at the 6-position of the diazapine ring, and a bromine is attached at the 8-position of the benzene ring .
Chemical Reactions Analysis
Flubrotizolam undergoes metabolism in the human body, with the main metabolic pathway being hydroxylation on the α- and/or 4-position mediated by CYP3A4 and CYP3A5, with subsequent glucuronidation of the hydroxylated metabolites as well as of the parent drug .
Physical And Chemical Properties Analysis
Flubrotizolam has a molecular weight of 377.24 g/mol . Its molecular formula is C15H10BrFN4S .
Scientific Research Applications
Study of New Psychoactive Substances (NPS)
Flubrotizolam has been used in the study of new psychoactive substances (NPS). It has been found that flubrotizolam-derived substances like clobromazolam and bromazolam have appeared on the drugs of abuse market . Research in this area helps in understanding the effects and risks associated with these new substances .
Clinical Use and Adverse Effects
As a tranquilizer, flubrotizolam has a wide range of clinical uses . It has been used in research to study its clinical and adverse effects . The most common effects noted by recreational users include heavy hypnosis and sedation, long-lasting amnesia, and rapid development of tolerance . Other effects include anxiolysis, muscle-relaxing effects, euphoria, loss of control, and severe withdrawals .
Study of Sleep Patterns
Flubrotizolam is a potent chemical compound utilized in scientific research to study sleep patterns. Given its sedative properties, it can be used to understand the mechanisms of sleep and the effects of sleep deprivation.
Examination of Anxiety-related Disorders
Flubrotizolam has been used in research to examine anxiety-related disorders. Its anxiolytic effects make it a useful tool for studying the neurobiology of anxiety and the efficacy of potential treatments.
Research on Drug Abuse
Flubrotizolam is a research chemical and novel benzodiazepine drug with effects similar to brotizolam . Its high potency makes it a common adulterant in other grey-market benzodiazepine preparations . Therefore, it has been used in research to study patterns of drug abuse and the risks associated with the use of adulterated drugs .
Mechanism of Action
Flubrotizolam, also known as ZWK85P59MH, is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects . This article will delve into the mechanism of action of Flubrotizolam, discussing its primary targets, mode of action, biochemical pathways, pharmacokinetics, results of action, and the influence of environmental factors on its action.
Target of Action
Flubrotizolam primarily targets the GABA-A receptors in the brain . GABA (gamma-aminobutyric acid) is an inhibitory neurotransmitter that reduces neuronal excitability. The GABA-A receptor is a type of GABA receptor that, when activated, allows the influx of chloride ions into the neuron, leading to hyperpolarization and decreased neuronal excitability .
Mode of Action
Flubrotizolam acts as a positive allosteric modulator of the GABA-A receptors . It enhances the effect of GABA by increasing the frequency of the chloride ion channel openings within the receptor . This leads to an influx of chloride ions, causing the neuron to become more negatively charged and thus less likely to generate an action potential . This results in a decrease in neuronal excitability, which manifests as sedative and anxiolytic effects .
Biochemical Pathways
The primary biochemical pathway affected by Flubrotizolam is the GABAergic system . By enhancing the action of GABA at the GABA-A receptors, Flubrotizolam increases inhibitory neurotransmission in the brain . This leads to a decrease in neuronal excitability and results in the calming and sedative effects characteristic of this compound .
Pharmacokinetics
Flubrotizolam is metabolized in the liver by an oxidative process carried out by the CYP450 enzyme family , particularly by CYP3A4 .
Result of Action
The primary result of Flubrotizolam’s action is a reduction in anxiety and induction of sedation . By enhancing GABAergic neurotransmission, Flubrotizolam slows down racing thoughts, reduces anxiety, and helps users fall asleep . This same effect also inhibits other aspects of brain function, including memory formation, abstract thinking, and decision-making .
Action Environment
The action of Flubrotizolam can be influenced by various environmental factors. For instance, the presence of other substances, such as alcohol or other CNS depressants, can potentiate the effects of Flubrotizolam, leading to increased sedation and potentially harmful effects . Additionally, individual factors such as age, health status, and genetic variations in the metabolizing enzymes can also influence the compound’s action, efficacy, and stability .
properties
| CAS RN | 57801-95-3 | Source  |
|---|
Retrosynthesis Analysis
AI-Powered Synthesis Planning: Our tool employs the Template_relevance Pistachio, Template_relevance Bkms_metabolic, Template_relevance Pistachio_ringbreaker, Template_relevance Reaxys, Template_relevance Reaxys_biocatalysis model, leveraging a vast database of chemical reactions to predict feasible synthetic routes.
One-Step Synthesis Focus: Specifically designed for one-step synthesis, it provides concise and direct routes for your target compounds, streamlining the synthesis process.
Accurate Predictions: Utilizing the extensive PISTACHIO, BKMS_METABOLIC, PISTACHIO_RINGBREAKER, REAXYS, REAXYS_BIOCATALYSIS database, our tool offers high-accuracy predictions, reflecting the latest in chemical research and data.
Strategy Settings
| Precursor scoring | Relevance Heuristic |
|---|---|
| Min. plausibility | 0.01 |
| Model | Template_relevance |
| Template Set | Pistachio/Bkms_metabolic/Pistachio_ringbreaker/Reaxys/Reaxys_biocatalysis |
| Top-N result to add to graph | 6 |
Feasible Synthetic Routes
Flubrotizolam (2-bromo-4-(2-fluorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine) is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects, which has been sold as a designer drug.
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Flubrotizolam
Cat. No. B3025693
CAS RN: 57801-95-3
M. Wt: 377.2 g/mol
InChI Key: VOZDBDBHBXLWCG-UHFFFAOYSA-N
Attention: For research use only. Not for human or veterinary use.
In StockQuick InquiryAdd To Inquiry Basket
- Click on QUICK INQUIRY to receive a quote from our team of experts.
- With the quality product at a COMPETITIVE price, you can focus more on your research.
Overview
2. Scientific research applications
Description
Flubrotizolam is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects . It has been sold as a designer drug . The IUPAC name for Flubrotizolam is 4-bromo-7-(2-fluorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.0 2,6]trideca-2(6),4,7,10,12-pentaene .
Molecular Structure Analysis
Flubrotizolam has a complex molecular structure. It is composed of a benzene ring fused to a seven-triazole membered 1,4-diazepine ring that is also fused to a 1,2,4 ring . An alkyl methyl (-CH3) is attached at the 1-position of the triazole ring, a 2-fluorophenyl ring is attached at the 6-position of the diazapine ring, and a bromine is attached at the 8-position of the benzene ring .
Chemical Reactions Analysis
Flubrotizolam undergoes metabolism in the human body, with the main metabolic pathway being hydroxylation on the α- and/or 4-position mediated by CYP3A4 and CYP3A5, with subsequent glucuronidation of the hydroxylated metabolites as well as of the parent drug .
Physical And Chemical Properties Analysis
Flubrotizolam has a molecular weight of 377.24 g/mol . Its molecular formula is C15H10BrFN4S .
Scientific Research Applications
Study of New Psychoactive Substances (NPS)
Flubrotizolam has been used in the study of new psychoactive substances (NPS). It has been found that flubrotizolam-derived substances like clobromazolam and bromazolam have appeared on the drugs of abuse market . Research in this area helps in understanding the effects and risks associated with these new substances .
Clinical Use and Adverse Effects
As a tranquilizer, flubrotizolam has a wide range of clinical uses . It has been used in research to study its clinical and adverse effects . The most common effects noted by recreational users include heavy hypnosis and sedation, long-lasting amnesia, and rapid development of tolerance . Other effects include anxiolysis, muscle-relaxing effects, euphoria, loss of control, and severe withdrawals .
Study of Sleep Patterns
Flubrotizolam is a potent chemical compound utilized in scientific research to study sleep patterns. Given its sedative properties, it can be used to understand the mechanisms of sleep and the effects of sleep deprivation.
Examination of Anxiety-related Disorders
Flubrotizolam has been used in research to examine anxiety-related disorders. Its anxiolytic effects make it a useful tool for studying the neurobiology of anxiety and the efficacy of potential treatments.
Research on Drug Abuse
Flubrotizolam is a research chemical and novel benzodiazepine drug with effects similar to brotizolam . Its high potency makes it a common adulterant in other grey-market benzodiazepine preparations . Therefore, it has been used in research to study patterns of drug abuse and the risks associated with the use of adulterated drugs .
Mechanism of Action
Flubrotizolam, also known as ZWK85P59MH, is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects . This article will delve into the mechanism of action of Flubrotizolam, discussing its primary targets, mode of action, biochemical pathways, pharmacokinetics, results of action, and the influence of environmental factors on its action.
Target of Action
Flubrotizolam primarily targets the GABA-A receptors in the brain . GABA (gamma-aminobutyric acid) is an inhibitory neurotransmitter that reduces neuronal excitability. The GABA-A receptor is a type of GABA receptor that, when activated, allows the influx of chloride ions into the neuron, leading to hyperpolarization and decreased neuronal excitability .
Mode of Action
Flubrotizolam acts as a positive allosteric modulator of the GABA-A receptors . It enhances the effect of GABA by increasing the frequency of the chloride ion channel openings within the receptor . This leads to an influx of chloride ions, causing the neuron to become more negatively charged and thus less likely to generate an action potential . This results in a decrease in neuronal excitability, which manifests as sedative and anxiolytic effects .
Biochemical Pathways
The primary biochemical pathway affected by Flubrotizolam is the GABAergic system . By enhancing the action of GABA at the GABA-A receptors, Flubrotizolam increases inhibitory neurotransmission in the brain . This leads to a decrease in neuronal excitability and results in the calming and sedative effects characteristic of this compound .
Pharmacokinetics
Flubrotizolam is metabolized in the liver by an oxidative process carried out by the CYP450 enzyme family , particularly by CYP3A4 .
Result of Action
The primary result of Flubrotizolam’s action is a reduction in anxiety and induction of sedation . By enhancing GABAergic neurotransmission, Flubrotizolam slows down racing thoughts, reduces anxiety, and helps users fall asleep . This same effect also inhibits other aspects of brain function, including memory formation, abstract thinking, and decision-making .
Action Environment
The action of Flubrotizolam can be influenced by various environmental factors. For instance, the presence of other substances, such as alcohol or other CNS depressants, can potentiate the effects of Flubrotizolam, leading to increased sedation and potentially harmful effects . Additionally, individual factors such as age, health status, and genetic variations in the metabolizing enzymes can also influence the compound’s action, efficacy, and stability .
properties
| CAS RN | 57801-95-3 | Source |
|---|
Retrosynthesis Analysis
AI-Powered Synthesis Planning: Our tool employs the Template_relevance Pistachio, Template_relevance Bkms_metabolic, Template_relevance Pistachio_ringbreaker, Template_relevance Reaxys, Template_relevance Reaxys_biocatalysis model, leveraging a vast database of chemical reactions to predict feasible synthetic routes.
One-Step Synthesis Focus: Specifically designed for one-step synthesis, it provides concise and direct routes for your target compounds, streamlining the synthesis process.
Accurate Predictions: Utilizing the extensive PISTACHIO, BKMS_METABOLIC, PISTACHIO_RINGBREAKER, REAXYS, REAXYS_BIOCATALYSIS database, our tool offers high-accuracy predictions, reflecting the latest in chemical research and data.
Strategy Settings
| Precursor scoring | Relevance Heuristic |
|---|---|
| Min. plausibility | 0.01 |
| Model | Template_relevance |
| Template Set | Pistachio/Bkms_metabolic/Pistachio_ringbreaker/Reaxys/Reaxys_biocatalysis |
| Top-N result to add to graph | 6 |
Feasible Synthetic Routes
7-Bromo-5-(2-fluorophenyl)-1,3-dihydrothieno[2,3-e][1,4]diazepin-2-one
Flubrotizolam
Reactant of Route 2
Flubrotizolam
Reactant of Route 3
Flubrotizolam
Reactant of Route 4
Flubrotizolam
Reactant of Route 5
Flubrotizolam
Reactant of Route 6
Flubrotizolam
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