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Meclonazepam
Meclonazepam ((''S'')-3-methylclonazepam) was discovered by a team at Hoffmann-La Roche in the 1970s and is a drug which is a benzodiazepine derivative similar in structure to clonazepam. It has sedative and anxiolytic actions like those of other benzodiazepines, and also has anti-parasitic effects against the parasitic worm ''Schistosoma mansoni''. Meclonazepam was never used as medicine and instead appeared online as a designer drug. Legal Issues United Kingdom In the UK, meclonazepam has been classified as a Class C drug by the May 2017 amendment to The Misuse of Drugs Act 1971 along with several other designer benzodiazepine drugs. See also * 3-Hydroxyphenazepam * Desmethylflunitrazepam * Nifoxipam * Oxazepam * Phenazepam * Ro05-4082 * SH-I-048A SH-I-048A (SH-i-048A) is a benzodiazepine derivative related in structure to compounds such as flubromazepam and meclonazepam. SH-I-048A is described as a non subtype selective superagonist at the benzodiazepine site ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hoffmann-La Roche
F. Hoffmann-La Roche AG, commonly known as Roche, is a Swiss multinational healthcare company that operates worldwide under two divisions: Pharmaceuticals and Diagnostics. Its holding company, Roche Holding AG, has shares listed on the SIX Swiss Exchange. The company headquarters are located in Basel. Roche is the fifth largest pharmaceutical company in the world by revenue, and the leading provider of cancer treatments globally. The company controls the American biotechnology company Genentech, which is a wholly owned affiliate, and the Japanese biotechnology company Chugai Pharmaceuticals, as well as the United States-based companies Ventana and Foundation Medicine. Roche's revenues during fiscal year 2020 were 58.32 billion Swiss francs. Descendants of the founding Hoffmann and Oeri families own slightly over half of the bearer shares with voting rights (a pool of family shareholders 45%, and Maja Oeri a further 5% apart), with Swiss pharma firm Novartis owning a furth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nifoxipam
Nifoxipam (3-hydroxydesmethylflunitrazepam, DP 370) is a benzodiazepine that is a minor metabolite of flunitrazepam and has been sold online as a designer drug. Nifoxipam produces strong tranquillising and sleep-prolonging effects and has much lower toxicity compared to lormetazepam and flunitrazepam in mice. See also * List of benzodiazepine designer drugs * Nitrazolam * Nitemazepam * Phenazepam Phenazepam (also known in Russia as bromdihydrochlorphenylbenzodiazepine) is a benzodiazepine drug, which was developed in the Soviet Union in 1975, and now produced in Russia and some CIS countries. Phenazepam is used in the treatment of vari ... References Designer drugs Fluoroarenes GABAA receptor positive allosteric modulators Glycine receptor antagonists Lactams Nitrobenzodiazepines Lactims {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABAA Receptor Positive Allosteric Modulators
In pharmacology, GABAA receptor positive allosteric modulators are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system. GABA is a major inhibitory neurotransmitter in the central nervous system. Upon binding, it triggers the GABAA receptor to open its chloride channel to allow chloride ions into the neuron, making the cell hyperpolarized and less likely to fire. GABAA PAMs increase the effect of GABA by making the channel open more frequently or for longer periods. However, they have no effect if GABA or another agonist is not present. Unlike GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-Aminobutyric acid (GABA) neurotransmitter molecule: they affect the receptor by binding at a different site on the protein. This is called allosteric modulation. In psychopharmacology, GABAA receptor PAMs used as drugs have mainly sedative and anxiolytic effects. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Designer Drugs
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects, and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human trials, the use of some of these drugs may result i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chloroarenes
In organic chemistry, an aryl halide (also known as haloarene) is an aromatic compound in which one or more hydrogen atoms, directly bonded to an aromatic ring are replaced by a halide. The haloarene are different from haloalkanes because they exhibit many differences in methods of preparation and properties. The most important members are the aryl chlorides, but the class of compounds is so broad that there are many derivatives and applications. Preparation The two main preparatory routes to aryl halides are direct halogenation and via diazonium salts. Direct halogenation In the Friedel-Crafts halogenation, Lewis acids serve as catalysts. Many metal chlorides are used, examples include iron(III) chloride or aluminium chloride. The most important aryl halide, chlorobenzene is produced by this route. Monochlorination of benzene is always accompanied by formation of the dichlorobenzene derivatives. Arenes with electron donating groups react with halogens even in the absence of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SH-I-048A
SH-I-048A (SH-i-048A) is a benzodiazepine derivative related in structure to compounds such as flubromazepam and meclonazepam. SH-I-048A is described as a non subtype selective superagonist at the benzodiazepine site of GABAA receptors, with a binding affinity of 0.77nM at the α1 subtype, 0.17nM at α2, 0.38nM at α3 and 0.11nM at α5. It has been used to study the functional differences between the different subtypes of the GABAA receptor. See also * GL-II-73 * QH-II-66 QH-II-66 (QH-ii-066) is a sedative drug which is a benzodiazepine derivative. It produces some of the same effects as other benzodiazepines, but is much more selective than most other drugs of this class and so produces somewhat less sedation a ... * SH-053-R-CH3-2'F References {{GABAAR PAMs Benzodiazepines GABAA receptor positive allosteric modulators ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ro05-4082
Ro05-4082 (N-methylclonazepam, ID-690) is a benzodiazepine derivative developed in the 1970s. It has sedative and hypnotic properties, and has around the same potency as clonazepam itself. It was never introduced into clinical use. It is a structural isomer of meclonazepam (3-methylclonazepam), and similarly has been sold as a designer drug, first being identified in Sweden in 2017. See also * Clonazolam * Cloniprazepam * Flunitrazepam Flunitrazepam, also known as Rohypnol among other names, is a benzodiazepine used to treat severe insomnia and assist with anesthesia. As with other hypnotics, flunitrazepam has been advised to be prescribed only for short-term use or by those ... References {{sedative-stub Abandoned drugs Pharmacology Nervous system Designer drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenazepam
Phenazepam (also known in Russia as bromdihydrochlorphenylbenzodiazepine) is a benzodiazepine drug, which was developed in the Soviet Union in 1975, and now produced in Russia and some CIS countries. Phenazepam is used in the treatment of various mental disorders such as psychiatric schizophrenia and anxiety. It can be used as a premedication before surgery as it augments the effects of anesthetics. Recently, phenazepam has gained popularity as a recreational drug; misuse has been reported in the United Kingdom, Finland, Sweden, and the United States. Indications * Neurosis, neurosis-like, psychopathic (personality disorder), psychopathic-like and other conditions accompanied by fear, anxiety, increased irritability, and emotional lability * Brief reactive psychosis and hypochondriasis-senestopathic syndrome * Vegetative dysfunction and vegetative lability * Insomnia * Alcohol withdrawal syndrome * Temporal lobe epilepsy and myoclonic epilepsy (used only occasionally as better ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxazepam
Oxazepam is a short-to-intermediate-acting benzodiazepine. Oxazepam is used for the treatment of anxiety and insomnia and in the control of symptoms of alcohol withdrawal syndrome. It is a metabolite of diazepam, prazepam, and temazepam, and has moderate amnesic, anxiolytic, anticonvulsant, hypnotic, sedative, and skeletal muscle relaxant properties compared to other benzodiazepines. It was patented in 1962 and approved for medical use in 1964. Medical uses It is an intermediate-acting benzodiazepine with a slow onset of action, so it is usually prescribed to individuals who have trouble staying asleep, rather than falling asleep. It is commonly prescribed for anxiety disorders with associated tension, irritability, and agitation. It is also prescribed for drug and alcohol withdrawal, and for anxiety associated with depression. Physicians may use oxazepam outside its approved indications to treat social phobia, post-traumatic stress disorder, insomnia, premenstrual syndrome, a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Desmethylflunitrazepam
Desmethylflunitrazepam (also known as norflunitrazepam, Ro05-4435 and fonazepam) is a benzodiazepine that is a metabolite of flunitrazepam and has been sold online as a designer drug. It has an IC50 value of 1.499 nM for the GABAA receptor. See also * Nitrazolam * Phenazepam * List of benzodiazepine designer drugs The below tables contain a sample list of benzodiazepines and benzodiazepine Analog (chemistry), analogs that are commonly prescribed, with their basic pharmacological characteristics, such as half-life and equivalent doses to other benzodiazepine ... References Designer drugs Fluoroarenes GABAA receptor positive allosteric modulators Glycine receptor antagonists Lactams Nitrobenzodiazepines {{sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzodiazepine
Benzodiazepines (BZD, BDZ, BZs), sometimes called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, insomnia, and seizures. The first benzodiazepine, chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955 and was made available in 1960 by Hoffmann–La Roche, who soon followed with diazepam (Valium) in 1963. By 1977, benzodiazepines were the most prescribed medications globally; the introduction of selective serotonin reuptake inhibitors (SSRIs), among other factors, decreased rates of prescription, but they remain frequently used worldwide. Benzodiazepines are depressants that enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABAA receptor, resulting in sedative, hypnotic ( sleep-inducing), anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant properties. High doses o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
3-Hydroxyphenazepam
3-Hydroxyphenazepam is a benzodiazepine with hypnotic, sedative, anxiolytic, and anticonvulsant properties. It is an active metabolite of phenazepam, as well as the active metabolite of the benzodiazepine prodrug cinazepam. Relative to phenazepam, 3-hydroxyphenazepam has diminished myorelaxant properties, but is about equivalent in most other regards. Like other benzodiazepines, 3-hydroxyphenazepam behaves as a positive allosteric modulator of the benzodiazepine site of the GABAA receptor with an EC50 value of 10.3 nM. It has been sold online as a designer drug. See also * Lorazepam, licensed medication * Nifoxipam Nifoxipam (3-hydroxydesmethylflunitrazepam, DP 370) is a benzodiazepine that is a minor metabolite of flunitrazepam and has been sold online as a designer drug. Nifoxipam produces strong tranquillising and sleep-prolonging effects and has much l ... * Nitemazepam References Hypnotics Anticonvulsants Sedatives Anxiolytics Benzodiazepines GABAA r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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