cas: 1261169-50-9 methyl 4-((hydroxyimino)methyl)-2-methylbenzoate
cas: 1261169-50-9 methyl 4-((hydroxyimino)methyl)-2-methylbenzoate
CBNumber: CB44844136
Chemical Name: methyl 4-((hydroxyimino)methyl)-2-methylbenzoate
Molecular Formula: C10H11NO3
Formula Weight: 193.2
CAS No.: 1261169-50-9
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CAS : 947331-05-7 Allisartan Isoproxil
CAS : 947331-05-7 Allisartan Isoproxil
CBNumber: CB03159860
Chemical Name: Allisartan Isoproxil
Molecular Formula: C27H29ClN6O5
Formula Weight: 553.01
CAS : 947331-05-7
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cas: 1272719-00-2 Pyrilutamide Anti-Hair Loss Treatment KX-826
cas: 1272719-00-2 Pyrilutamide Anti-Hair Loss Treatment KX-826
CBNumber: CB88252856
Chemical Name: Benzamide, 4-[3-[4-cyano-2-fluoro-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methyl-
Molecular Formula: C21H15F5N4O2S
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CAS : 60951-19-1 NEDPA EPE Ephenidine Benzeneethanamine
CAS : 60951-19-1 NEDPA EPE Ephenidine Benzeneethanamine
CBNumber: CB23170498
Chemical Name: Benzeneethanamine, N-ethyl-a-phenyl-
Molecular Formula: C16H19N
Formula Weight: 225.33
CAS No.: 60951-19-1
cas: 4919-33-9 4-ethoxyphenylacetic acid
cas: 4919-33-9 4-ethoxyphenylacetic acid
CBNumber: CB2174653
Chemical Name: 4-ETHOXYPHENYLACETIC ACID
Molecular Formula: C10H12O3
Formula Weight: 180.2
CAS No.: 4919-33-9
cas: 15690-57-0 Enclomiphene
cas: 15690-57-0 Enclomiphene
CBNumber: CB8128416
Chemical Name: TRANS-CLOMIPHENE HCL
Molecular Formula: C26H28ClNO
Formula Weight: 405.96
CAS No.: 15690-57-0
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cas: 915759-54-4 WAY-316606
cas: 915759-54-4 WAY-316606
CBNumber: CB82627535
Chemical Name: BenzenesulfonaMide, 5-(phenylsulfonyl)-N-4-piperidinyl-2-(trifluoroMethyl)-
Molecular Formula: C18H19F3N2O4S2
Formula Weight: 448.4796696
CAS No.: 915759-45-4
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cas: 774118-46-6 NPDPA
cas: 774118-46-6 NPDPA
CBNumber: CB69806955
Chemical Name: Benzeneethanamine, N-(1-methylethyl)-α-phenyl-
Molecular Formula: C17H21N
Formula Weight:
CAS No.: 774118-46-6
cas: 12279-41-3 Seractide ACTH(1-39),human
cas: 12279-41-3 Seractide ACTH(1-39),human
CBNumber: CB3318698
Chemical Name: Seractide ACTH(1-39),human
Molecular Formula: C207H308N56O58S1
Formula Weight: 4541.07
CAS No.: 12279-41-3
cas: 77465-10-2 ACTH (1-39) (mouse,rat) ADRENOCORTICOTROPIC HORMONE RAT
cas: 77465-10-2 ACTH (1-39) (mouse,rat) ADRENOCORTICOTROPIC HORMONE RAT
CBNumber: CB8102054
Chemical Name: ADRENOCORTICOTROPIC HORMONE RAT
Molecular Formula: C210H315N57O57S1
Formula Weight: 4582.16
CAS No.: 77465-10-2
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cas: 191936-91-1 HIV-1 TAT Protein Peptide
cas: 191936-91-1 HIV-1 TAT Protein Peptide
CBNumber: CB0115759
cas: 191936-91-1 HIV-1 TAT Protein Peptide
Molecular Formula: C64H118N32O14
Formula Weight: 1559.83
CAS No.: 191936-91-1
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cas: 230299-95-3 Apelin-36 (rat, mouse)
cas: 230299-95-3 Apelin-36 (rat, mouse)
CBNumber: CB3669112
cas: 230299-95-3 Apelin-36 (rat, mouse)
Molecular Formula: C185H304N68O43S
Formula Weight:
CAS No.: 230299-95-3
cas: 28319-77-9 Alpha-GPC Chonile Alfoscerate L-Alpha glycerylphosphorylcholine
cas: 28319-77-9 Alpha-GPC Chonile Alfoscerate L-Alpha glycerylphosphorylcholine
Alpha GPC (L-Alpha Glycerylphosphorylcholine, choline alfoscerate) is a choline source derived from soy or sunflower lecithin. It is also naturally present in small amounts in your body.
Alpha GPC is more bioavailable than other sources of choline for brain benefits. Unlike choline citrate or choline bitartrate, it easily crosses the blood-brain barrier. This makes Alpha GPC a preferred choline source with experienced nootropic users.
Alpha GPC is a precursor to the essential neurotransmitter acetylcholine.
Alpha GPC helps:
Brain Energy. Alpha GPC improves mood, and boosts mental energy. The extra choline can increase alertness and clarity of thought.
Neurotransmitters. Alpha GPC is prized for its ability to improve memory. Its high bioavailability makes it a great source of choline for producing the neurotransmitter acetylcholine.
Brain Optimization. Alpha GPC boosts the development of new brain cells. And enhances your brain’s ability to repair damaged cell membranes.
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cas: 72432-10-1 aniracetam factory Manufactory supplier lab laboratory wholesaler retailer
cas: 72432-10-1 aniracetam factory Manufactory supplier lab laboratory wholesaler retailer
Aniracetam is a compound in the group of racetams due to its common pyrrolidone structure. It is one of the more common Racetamic structures. It is fat-soluble and thus needs to be ingested with fatty acids. Additionally, Aniracetam is cholinergic
Aniracetam acts as a positive modulator of some excitatory receptors known as AMPA receptors and decreases the rate of receptor desensitization. This typically manifests as a controlled and prolonged neurological stimulation effect. Since AMPA receptors differ in structure across the brain, different AMPA modulators affect the brain in different ways.
Anecdotally, aniracetam has been know to aid in 'collective and holistic thinking', or putting the pieces of the puzzle together. It also increases blood flow and activity in the area of the brain known for this action, the association cortex.
Aniracetam, as an AMPA modulator, is currently being studied for usage in depression and other CNS disorders such as Alzheimer's disease.
Nootropics like Aniracetam have the power to improve your cognitive and mental performance abilities in a way that few other substances can replicate. Aniracetam is one of the most popular options on the market, and countless members of the nootropic community swear by its ability to improve their focus, memory retention, and mood.
If you’ve done any research on aniracetam or other nootropics, you’ve probably already read tons of anecdotal evidence and user reviews. However, as a beginner, how do you know the best way to get started? Today, we’ll cover everything you need to know about aniracetam including the dosage
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cas: 14610-11-8 Bemethyl Bemethyl Synthetic Adaptogen Bromantane Alternative
cas: 14610-11-8 Bemethyl Bemethyl Synthetic Adaptogen Bromantane Alternative
CBNumber: CB71292876
Chemical Name: 1H-Benzimidazole,2-(ethylthio)-(9CI)
Molecular Formula: C9H10N2S
Formula Weight: 178.25
CAS No.: 14610-11-8
Bemethyl, also commonly referred to in literature as bemitil, is a synthetic actoprotector which is also antihypoxant (combating conditions of hypoxia), antioxidant, and antimutagenic.
It resists metabolization and is long-lived, accumulating in tissues over course of treatment. In one study involving rats, long-term administration of Bemethyl was accompanied by a 1.38-fold increase in drug concentration in the brain, and a 1.68-fold increase in its concentration in skeletal muscles.[9]
The chemical structure of the powder is similar to that of nucleobases adenine and guanine, which can explain its pharmacological effects. The compound does increase the expression of RNA and proteins in the skeletal muscle, brain cells, liver, and kidneys. It also stimulates ATP formation and gluconeogenesis. Gluconeogenesis is the process of formation of glucose from non-carbohydrate substrates, such as lactate, fats and glucogenic amino acids
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cas: 19608-29-8 CB-03-01 BREEZULA Hair Loss Cure
cas: 19608-29-8 CB-03-01 BREEZULA Hair Loss Cure
What is CB-03-01?
CB-03-01 (cortexolone 17α-propionate, CB0301) 1% cream is a topical androgen receptor inhibitor which has mainly been developed for the treatment of acne vulgaris (1). It is also presently being investigated in a large phase II clinical trial for the topical treatment of male-pattern baldness. CB-03-01 has been found to inhibit the androgen receptor regulated pathway (1). Also known as clascoterone, CB-03-01 is being developed by Cassiopea (a spin-off company from Cosmo Pharmaceuticals) and was initially commercialised as Breezula. Data from 2020 reveal that clascoterone is also being marketed as Winlevi for the management of acne vulgaris. CB-03-01 is thought to compete with DHT for its binding to androgen receptors in both the sebaceous gland and dermal papilla cells within hair follicles. The difference between Winlevi and Breezula is that Breezula is a solution that contains a higher concentration of the drug for the treatment of male-pattern baldness(2). In 2019, Cassiopea announced positive phase II 12-month results for their flagship product Breezula in the management of androgenetic alopecia. The phase II clinical trial recruited in excess of 400 participants in Germany and sought to evaluate the efficacy and safety of 4 different dosing regimens of CB-03-01 compared to vehicle agents in male subjects between the ages of 18 and 55 with mild to moderate male-pattern baldness. All participants were randomised to either apply CB-03-01 or a vehicle agent to balding areas of the scalp daily for 12 months. 5 treatment groups were analysed – 2.5% solution twice-daily, 5.0% solution twice-daily, 7.5% solution twice-daily, 7.5% solution once-daily, and vehicle solution twice-daily.
Researchers used target area hair count (TAHC) and hair growth assessment (HGA) score as the primary end-points of interest. For TAHC, statistically significant changes versus the vehicle agent were observed in all of the active treatment groups, with the most significant improvements observed in the 7.5% twice-daily
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CAS: 138112-76-2 Agomelatine factory Manufactory supplier lab laboratory wholesaler retailer
CAS: 138112-76-2 Agomelatine factory Manufactory supplier lab laboratory wholesaler retailer
Agomelatine is an antidepressant medication used in the treatment of depression (a mood disorder that involves persistent feelings of sadness and loss of interest in daily activities) in adults. Agomelatine works by increasing the levels of a chemical substance in your brain, which helps to improve mood and reduce the feeling of anxiety. Agomelatine causes side effects such as nausea, diarrhoea or constipation, headache, drowsiness, dizziness, changes in the sleeping pattern, increased levels of liver enzymes, and tiredness. Consult your doctor if these symptoms persist or worsen. Avoid taking this medicine if you are allergic to it. Agomelatine may be taken with or without food as directed by your doctor. Take it at the same time every day for the ease of remembering. Do not stop taking Agomelatine without consulting your doctor, as it may cause withdrawal symptoms. Agomelatine can alter your mood and cause suicidal thoughts. Therefore, closely observe for any change in your mood or behaviour while you take this medicine. Consult your doctor immediately if you experience such symptoms. Agomelatine is not recommended for use if you have active liver problems as it may further worsen your condition. Also, inform your doctor if you are taking any other medications or have any other medical conditions to avoid undesired effects. Agomelatine is not recommended for use in children below 18 years of age and the elderly above 65 years of age as the safety and efficacy data are not clinically established. Consult your doctor if you are pregnant or are breastfeeding.
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cas: 1076225-26-7 (rac)-PF-998425
cas: 1076225-26-7 (rac)-PF-998425
(Rac)-PF-998425 is a potent, selective, nonsteroidal androgen receptor (AR) antagonist. (Rac)-PF-998425 has IC50 values of 26 and 90 nM in the AR binding and cellular assays, respectively. (Rac)-PF-998425 has the potential for the research of the androgenetic alopecia
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cas: 90357-06-5 Bicalutamide
cas: 90357-06-5 Bicalutamide
Bicalutamide is used together with a luteinizing hormone releasing hormone (LHRH) analog (eg, goserelin or leuprolide) to treat stage D2 metastatic prostate cancer (cancer that has spread) in men. Bicalutamide belongs to the group of medicines called antiandrogens. It works by blocking the effects of testosterone (a male hormone), which helps stop the growth and spread of cancer cells.
How to use Bicalutamide
Read the Patient Information Leaflet if available from your pharmacist before you start taking bicalutamide and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
Take this medication by mouth with or without food as directed by your doctor, usually once a day.
Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.
Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.
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cas: 1030377-33-3 suvorexant MK-4305 MK4305
cas: 1030377-33-3 suvorexant MK-4305 MK4305
Suvorexant is used treat insomnia (difficulty falling asleep or staying asleep). Suvorexant is in a class of medications called orexin receptor antagonists. It works by blocking the action of a certain natural substance in the brain that causes wakefulness.
Suvorexant comes as a tablet to take by mouth. It is usually taken once a day, if needed, no earlier than 30 minutes before bedtime. Suvorexant may be taken with or without food but will begin to work faster if taken on an empty stomach. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take suvorexant exactly as directed. Never take more than one dose of suvorexant per day even if you are still having trouble falling asleep or staying asleep.
You will probably become very sleepy soon after you take suvorexant and will remain sleepy for some time after you take the medication. Plan to go to bed right after you take the medication and to stay in bed for at least 7 hours. Do not take suvorexant if you will be unable to remain asleep for the required number of hours after taking the medication. If you get up too soon after taking suvorexant, you may experience drowsiness and difficulty driving or performing tasks that require alertness.
Your sleep problems should improve within 7 to 10 days after you start taking suvorexant. Call your doctor if your sleep problems do not improve during this time or if they get worse at any time during your treatment.
Your doctor will probably start you on a low dose of suvorexant and may gradually increase your dose if your insomnia does not improve. Your doctor may also decrease your dose of suvorexant or tell you to stop taking the medication if it makes you feel too drowsy during the day.
Swallow the tablets whole; do not split, chew, or crush them.
Suvorexant may be habit forming. Do not take a larger dose, take it more often, or take it for a longer period of time than prescribed by your doctor.
Suvorexant, sold under the brand name Belsomra, is an orexin antagonist medication which is used in the treatment of insomnia.It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset and/or maintenance in adults. Suvorexant helps with falling asleep faster, sleeping longer, being awake less in the middle of the night, and having better quality of sleep. Its effectiveness is modest, and is similar to that of other orexin antagonists, but is lower than that of benzodiazepines and Z-drugs. Suvorexant is taken by mouth
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cas: 1621169-52-5 ACE-031 Myostatin inhibitory peptide 7
cas: 1621169-52-5 ACE-031 Myostatin inhibitory peptide 7
ACE-031 is a soluble form of the type IIB activin receptor (ACVR2B), which is a potent regulator of muscle growth in vivo. Myostatin, a negative regulator of muscle growth, is bound by ACVR2B and subsequently inactivated. Research in mouse models shows that knocking out the activin receptor boosts mass in all muscle cells. As a result of this connection, ACE-031 has been investigated in several clinical trials as a potential treatment for muscle-wasting diseases like Duchenne muscular dystrophy (DMD). Activin receptors also play important roles in the development of gametocytes, particularly sperm. The receptor is also often found to be inactivated in prostate cancer and is damaged or dysfunctional in several different types of colorectal cancer.
What Is ACE-031?
ACE-031 is a soluble form of the activin type IIB receptor and is known to bind to myostatin and neutralize its effects. Myostatin is a protein, produced by muscle cells, that inhibits both hypertrophy and hyperplasia of skeletal muscle. ACE-031 also likely has effects on bone metabolism, fat storage, and the health of sperm.
ACE-031 Research and Muscle Protection After Menopause
ACE-031 was tested in a small clinical trial to determine if it could help to maintain muscle mass in postmenopausal, healthy women. Maintaining muscle is critical to long-term bone health and helps to reduce the rate of joint injuries, falls, etc. in both men and women as they age. In a small placebo-controlled trial, ACE-031 produced significant increases in both lean body mass and thigh muscle volume after just a single dose. Results were observed 29 days after the injection[1]. The study was particularly interesting because a secondary, unexpected outcome was observed. Trials participants receiving ACE-031 showed improvement in serum biomarkers of both bone and fat metabolism. This suggests that ACE-031, while primarily associated with muscle growth, likely inhibits fat storage and boosts bone production.
ACE-031 May Be Necessary for Maximum Muscle Cell Growth
Research in mice indicates that maximal skeletal muscle growth can only be attained with a myostatin inhibitor like ACE-031. Furthermore, it appears that blockade of myostatin by multiple avenues is most beneficial[2]. While these findings are preliminary, they suggest that maximum muscle protection in muscle-wasting conditions might require a multifaceted approach utilizing therapies that both boost growth (growth hormone, IGF-1) and reduce muscle wasting (ACE-031).
ACE-031 Research and Strength
There appears to be more to the ability of ACE-031 to improve muscle function than inhibition of myostatin. Research in mice indicates that ACE-031 can improve force-generating capacity in muscle tissue, in part by preserving energy supply and shifting muscle thermodynamics toward oxidative respiration. In the mice, administration of ACE-031 improved maximum and total contractile force by 40% and 25% respectively. There was no overall change in fatigue of muscle though, indicating that ACE-031 improves muscle strength without affecting energy dynamics. The research revealed no changes in ATP homeostasis or contractile efficiency[4].
ACE-031 Tested in Clinical Trials for Muscle Repair
Duchenne muscular dystrophy (DMD) is an x-linked recessive condition characterized by severe muscle loss. It generally leads to an inability to walk by age 12 with muscles that are lacking in protein content but that are exceptionally high in fat content. Due to a dysfunctional dystrophin protein, muscle cells in DMD are weak and prone to damage. Though this is the primary cause of the disease, a secondary effect occurs when myostatin leaks from damaged muscle cells and slows or inhibits growth in other cells. Gene therapy to address the dystrophin dysfunction has so far proved untenable, but there is currently hope that ACE-031 can slow the muscle damage by reducing the secondary impact caused by myostatin.
In a recent clinical trial, subcutaneous injection of ACE-031 every 2-4 weeks
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cas: 1088715-84-7 LY-2510924 LY2510924
cas: 1088715-84-7 LY-2510924 LY2510924
Molecular Formula: C62H88N14O10
Formula Weight: 1189.47
CAS No.: 1088715-84-7
cas: 3258-02-4 N(4)-hydroxycytidine EIDD-1931
cas: 3258-02-4 N(4)-hydroxycytidine EIDD-1931
N4-hydroxycytidine and its prodrug EIDD-2801 is being studied for its activity against a number of viral infections including influenza, MERS-CoV, and SARS-CoV-2
N4-Hydroxyctidine, or EIDD-1931, is a ribonucleoside analog which induces mutations in RNA virions.1,2 N4-hydroxycytidine was first described in the literature in 1980 as a potent mutagen of bacteria and phage.5 It has shown antiviral activity against Venezuelan equine encephalitis virus,1 and the human coronavirus HCoV-NL63 in vitro.4 N4-hydroxycytodine has been shown to inhibit SARS-CoV-2 as well as other human and bat coronaviruses in mice and human airway epithelial cells.3 It is orally bioavailable in mice and distributes into tissue before becoming the active 5’-triphosphate form, which is incorporated into the genome of new virions, resulting in the accumulation of inactivating mutations.2 In non-human primates, N4-hydroxycytidine was poorly orally bioavailable.6 A remdesivir resistant mutant mouse hepatitis virus has also been shown to have increased sensitivity to N4-hydroxycytidine.3 The prodrug of N4-hydroxycytidine, EIDD-2801, is also being investigated for its broad spectrum activity against the coronavirus family of viruses.3
N4-Hydroxycytidine (3258-02-4) was originally identified as a mutagen effecting AT to GC base-pair transitions.1 It has also been found to have antiviral properties against a broad range of viruses including hepatitis C2, norovirus3, Ebola virus4, Chikungunya virus5, influenza and respiratory syncytial viruses6, and importantly, coronaviruses.7,8 N4-hydroxycytidine is the active molecule in the antiviral pro-drug clinical candidate EIDD-2801
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cas: 85815-37-8 Rilmazafone Hydrochloride
cas: 85815-37-8 Rilmazafone Hydrochloride
CBNumber: CB02469946
Chemical Name: Rilmazafone Hydrochloride
Molecular Formula: C21H21Cl3N6O3
Formula Weight: 511.79
CAS No.: 85815-37-8
Rilmazafone Rhythmy, previously known as 450191-S is a water-soluble prodrug developed in Japan. Once metabolized, rilmazafone is converted into several benzodiazepine metabolites that have sedative and hypnotic effects These metabolites induce impairment of motor function and have hypnotic properties.
Rilmazafone is not a benzodiazepine, since there is no benzene ring fused with a diazepine ring in the compound; in fact, the parent drug has no diazepine ring. It is therefore not classified as a benzodiazepene in several countries, including the United States, where it is not designated a controlled substance. Rilmazafone has no effects on benzodiazepine receptors itself, nor does it produce any psychoactive effects prior to metabolism. However, once inside the body it is metabolized by aminopeptidase enzymes in the small intestine to form the principal active benzodiazepine 8-chloro-6-(2-chlorophenyl)-N,N-dimethyl-4H-1,2,4-triazolo [1,5-a]benzodiazepine-2-carboxamide.As can be seen in the molecular diagram below, the principal metabolite contains a benzodiazepine ring structure (i.e., a benzene ring fused with a diazepine ring), unlike the parent compound (rilmazafone), which has no diazepine ring
Rilmazafone induces impairment of motor function and has hypnotic properties. Rilmazafone has no effects on benzodiazepine receptors itself, but once inside the body is metabolised by aminopeptidase enzymes in the small intestine to form the active benzodiazepine 8-chloro-6-(2-chlorophenyl)-N,N-dimethyl-4H-1,2,4-triazolo benzodiazepine-2-carboxamide. Preclinical studies have shown its excellent effects inducing and maintaining sleep with little effect on the skeletal muscle. Earlier the clinical dose for this drug as a premedicant was found to be 2-4mg. Zolpidem Triazolam Rilmazafone Elderly Residual effects Randomized study,
Rilmazafone is considered to be a benzodiazepine pro-drug, and in Japan, is used for the short-term treatment of insomnia. Benzodiazepines are scheduled as Prescription Medicines in Schedule 1 of the Medicines Regulations 1984. However, rilmazafone is itself not a benzodiazepine.
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cas: 84379-13-5 Bretazenil factory low price
cas: 84379-13-5 Bretazenil factory low price
CBNumber: CB6503200
Chemical Name: Bretazenil
Molecular Formula: C19H20BrN3O3
Formula Weight: 418.28
CAS No.: 84379-13-5
Bretazenil (Ro16-6028) is an imidazopyrrolobenzodiazepine anxiolytic drug which is derived from the benzodiazepine family, and was invented in 1988. It is most closely related in structure to the GABA antagonist flumazenil, although its effects are somewhat different. It is classified as a high-potency benzodiazepine due to its high affinity binding to benzodiazepine binding sites where it acts as a partial agonist. Its profile as a partial agonist and preclinical trial data suggests that it may have a reduced adverse effect profile. In particular bretazenil has been proposed to cause a less strong development of tolerance and withdrawal syndrome. Bretazenil differs from traditional 1,4-benzodiazepines by being a partial agonist and because it binds to α1, α2, α3, α4, α5 and α6 subunit containing GABAA receptor benzodiazepine receptor complexes.
Bretazenil is an anxiolytic drug which is derived from the benzodiazepine family, and was invented in 1988. It is most closely related in structure to the benzodiazepine antagonist flumazenil, although its effects are somewhat different.
Bretazenil was originally developed as an anti-anxiety drug, but never commercialised. It is a partial agonist for GABAA receptors in the brain. David Nutt from the University of Bristol has suggested bretazenil as a possible base from which to make a better social drug, as it displays several of the positive effects of alcohol intoxication such as relaxation and sociability, but without the bad effects such as aggression, amnesia, nausea, loss of coordination, liver disease and brain damage. The effects of bretazenil can also be quickly reversed by the action of flumazenil, which is used as an antidote to benzodiazepine overdose, in contrast to alcohol for which there is no effective and reliable antidote.
However, while less addictive than benzodiazepine full agonists such as diazepam, long-term use of bretazenil would still be expected to result in dependence and addiction. Bretazenil, were it to be made commercially available, would thus most likely be classed as a controlled substance, e.g. Schedule III or Schedule IV in the USA, and so is unlikely to ever be commercialised for recreational use in that country. More liberal jurisdictions however might potentially permit the sale of bretazenil as a recreational alternative to alcohol, especially in countries such as Russia where liver and brain damage from chronic alcohol abuse place a severe burden on the health service and so the potential advantages of a less toxic alternative drug might outweigh the complications of introducing a new recreational drug to the market
The imidazobenzodiazepines bretazenil, imidazenil, and FG-8205 (Figure 10a) are high-affinity partial agonists for GABAA receptor subtypes that contain α1, α2, α3, and α5 subunits. These compounds are anxiolytic in animal models, with a greater separation between doses required for anxiolytic versus sedative effects than that observed for diazepam. Where studied, these compounds also show little evidence for tolerance to the anxiolytic effects, do not display withdrawal, and have a lower abuse potential than full BZ agonists in nonhuman primates. Bretazenil (Figure 10a) entered clinical studies in the mid-1980s and was efficacious in GAD and panic disorder,112 with a lower abuse potential than diazepam.113 However, bretazenil was sedative, with little evidence for separation between anxiolytic and sedative effects,114 and its clinical development was discontinued.
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