Bretazenil CAS: 84379-13-5

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Bretazenil (also known as Ro11-6896) is a chemical used in anti-anxiety medication, which acts as a selective GABA-A receptor agonist. GABA-A receptors are a subclass of the ionotropic receptors located in the brain that play a vital role in the inhibitory neurotransmitters that help lower anxiety levels and promote relaxation. Bretazenil has a molecular formula of C18H17N3O3 and is classified as a benzodiazepine drug, along with other well-known anti-anxiety medications like Ativan and Xanax. In this article, we will be discussing various aspects of Bretazenil, including its chemical properties, health benefits, potential effects and side effects, dosage information, and much more.

Chemical Name and Molecular Formula

Bretazenil has a chemical name of 7-(2,2-diphenyl-1-hydroxyethyl)-6-(2-propen-1-yl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid methyl ester. Its molecular formula is C18H17N3O3, and its molar mass is 323.34 g/mol.

CAS No.

The CAS No. or Chemical Abstracts Service Number of Bretazenil is 84379-13-5.

Top Searched Keywords on Google and Synonyms

The top searched keywords on Google for Bretazenil include:

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Some common synonyms for Bretazenil include Ro11-6896, MK-0677, L-79206, and 7-(2,2-Diphenyl-1-oxoethyl)-6-(3-propenyl)-4H,5H,6H,7H,8H-Imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid methyl ester.

Health Benefits

Bretazenil is a benzodiazepine drug that is primarily used for its anxiolytic or anti-anxiety effects. It helps in the treatment of various anxiety disorders, including generalized anxiety disorder and panic disorder. It also has sedative and hypnotic properties, which make it useful in treating insomnia or sleep disorders as well.

Potential Effects

Bretazenil acts as a selective GABA-A receptor agonist, which helps increase the levels of gamma-aminobutyric acid (GABA) in the brain. GABA is a neurotransmitter that works to reduce neuron excitability, thereby calming the nervous system and lowering anxiety levels. By binding to these receptors, Bretazenil helps promote relaxation and reduces fear and anxiety symptoms. It can also cause sedation and hypnosis in high doses.

Mechanisms

Bretazenil works by binding selectively to the GABA-A receptors, which are ligand-gated ion channels located in the brain. These receptors are involved in mediating the activity of GABA, which is the primary inhibitory neurotransmitter in the brain. GABA works by reducing neuron excitability, thereby helping to lower anxiety levels and promote relaxation. By binding to these receptors, Bretazenil facilitates the opening of chloride ion channels, which allows chloride ions to enter the neuron, making it harder to depolarize and reducing its firing rate. This reduces neuron activity and calms the nervous system.

Safety

Bretazenil is a prescription drug and should not be used without a doctor's approval. It should be used with caution in patients with a history of drug or alcohol abuse, liver or kidney problems, and respiratory or cardiovascular diseases. It is not recommended for use during pregnancy, as it can cause harm to the fetus. It is also not recommended for individuals who have previously experienced an allergic reaction to benzodiazepines.

Side-Effects

Bretazenil can cause a variety of side effects, ranging from mild to severe. The most common side effects include dizziness, drowsiness, lethargy, memory impairment, confusion, anxiety, and blurred vision. Other less common side effects include nausea, vomiting, dry mouth, headaches, and fatigue. In rare cases, it can cause an allergic reaction, which can lead to difficulty breathing, hives, or swelling of the face, lips, tongue, or throat. If you experience any of these side effects, contact your doctor immediately.

Dosage Information

The dosage of Bretazenil will vary depending on the severity of the condition being treated, the patient's age, weight, and medical history, and other factors. Your doctor will determine the appropriate dosage for you after considering your individual needs. It is essential to follow your doctor's instructions carefully and not exceed the recommended dosage, as this can lead to severe side effects.

Conclusion

Bretazenil is a benzodiazepine drug that is primarily used for the treatment of anxiety disorders, insomnia, and other sleep disorders. It acts as a selective GABA-A receptor agonist, which helps promote relaxation, reduce fear, and anxiety symptoms. It is essential to be careful when using this drug and to follow your doctor's instructions carefully to avoid any adverse effects that may occur.

Formula Weight ：418.3

Purity ：≥98%

Bretazenil is an anxiolytic drug that belongs to the benzodiazepine class.
Bretazenil has a broader action spectrum than traditional benzodiazepines. However, the partial agonist imidazenil does not act on these subunits. In terms of psychomotor impairment, 0.5mg of bretazenil is roughly equivalent to 10 mg of diazepam. When taken alone or in combination with alcohol, bretazenil has pronounced sedative-hypnotic effects. According to this human study, bretazenil may be more sedative than diazepam. The reason for this is unknown, but the study suggests that a full-agonist metabolite may be produced in humans but not previously tested animals, or that there are significant differences in the benzodiazepine receptor population in animals and humans.

Bretazenil is an anticonvulsant and anxiolytic GABAA receptor positive allosteric modulator. 1 It increases GABA-gated chloride currents in rat cortical neurons and HEK293 cells expressing GABAA receptors with 12 subunits (EC50s = 60 and 10 nM, respectively). 1 Bretazenil (IC50 = 2.2 nM) inhibits the binding of the benzodiazepine diazepam to rat cerebral cortex homogenates. 2 It prevents tonic convulsions in rats caused by pentylenetetrazol (PTZ; Item No. 18682) and maximal electroshock (MES) (ED50s = 0.07 and 0.48 mg/kg, respectively). In mice, bretazenil (5-30 mg/kg) increases the number of open arm entries and the percentage of time spent in open arms of the elevated plus maze, indicating anxiolytic-like activity.

Bretazenil was discovered to antagonize the effects of full agonist benzodiazepines in a monkey study. However, bretazenil has been shown to enhance the effects of neurosteroids acting on the GABAA receptor's neurosteroid binding site. Another study discovered that bretazenil acted as an antagonist in monkeys who were physically dependent on the full agonist benzodiazepine triazolam, causing withdrawal symptoms.