Fluadinazolam
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Fluadinazolam
Fluadinazolam is a benzodiazepine derivative developed in 1973, with sedative and anxiolytic effects. It is a derivative of the never commercially marketed benzodiazepine adinazolam and has similarly been sold as a designer drug. See also * Flualprazolam * Flubromazepam * Fluclotizolam Fluclotizolam is a thienotriazolodiazepine derivative which was first synthesised in 1979, but was never marketed. It has subsequently been sold as a designer drug, first being definitively identified in 2017. See also * Brotizolam * Clotizola ... * Fludiazepam * Flutemazepam References Designer drugs GABAA receptor positive allosteric modulators Fluoroarenes Heterocyclic compounds with 3 rings Nitrogen heterocycles Chloroarenes {{nervous-system-drug-stub ...
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Adinazolam
AdinazolamFR Patent 2248050 (marketed under the brand name Deracyn) is a tranquilizer of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. It possesses anxiolytic, anticonvulsant, sedative, and antidepressant properties. Adinazolam was developed by Jackson B. Hester, who was seeking to enhance the antidepressant properties of alprazolam, which he also developed. Adinazolam was never FDA approved and never made available to the public market, however it has been sold as a designer drug. Side effects Overdose may include muscle weakness, ataxia, dysarthria and particularly in children paradoxical excitement, as well as diminished reflexes, confusion and coma may ensue in more severe cases. A human study comparing the subjective effects and abuse potential of adinazolam (30 mg and 50 mg) with diazepam, lorazepam and a placebo showed that adinazolam causes the most "mental and physical sedation" and the greatest "mental un ...
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Flualprazolam
Flualprazolam is a tranquilizer of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. It was first synthesised in 1976, but was never marketed. It can be seen as the triazolo version of fludiazepam.It has subsequently been sold as a designer drug, first being definitively identified as such in Sweden in 2018. It can be described as the 2'-fluoro derivative of alprazolam or the fluoro instead of chloro analogue of triazolam, and has similar sedative and anxiolytic effects. Legal status Flualprazolam is banned in Sweden, also is illegal in the UK. In December 2019, the World Health Organization recommended flualprazolam for international scheduling as a Schedule IV medication under the Convention on Psychotropic Substances. The substance is illegal in Oregon.
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Fluclotizolam
Fluclotizolam is a thienotriazolodiazepine derivative which was first synthesised in 1979, but was never marketed. It has subsequently been sold as a designer drug, first being definitively identified in 2017. See also * Brotizolam * Clotizolam * Deschloroclotizolam * Etizolam * Flualprazolam * Fluadinazolam Fluadinazolam is a benzodiazepine derivative developed in 1973, with sedative and anxiolytic effects. It is a derivative of the never commercially marketed benzodiazepine adinazolam and has similarly been sold as a designer drug. See also * Fl ... * Flubrotizolam * Fluetizolam * Ro09-9212 References {{GABAAR PAMs Designer drugs GABAA receptor positive allosteric modulators Thienotriazolodiazepines ...
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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 ...
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Sedative
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are CNS depressants and interact with brain activity causing its deceleration. Various kinds of sedatives can be distinguished, but the majority of them affect the neurotransmitter gamma-aminobutyric acid (GABA). In spite of the fact that each sedative acts in its own way, most produce relaxing effects by increasing GABA activity. This group is related to hypnotics. The term ''sedative'' describes drugs that serve to calm or relieve anxiety, whereas the term ''hypnotic'' describes drugs whose main purpose is to initiate, sustain, or lengthen sleep. Because these two functions frequently overlap, and because drugs in this class generally produce dose-dependent effects (ranging from anxiolysis to loss of consciousness) they are often referred to collectively as ''sedative-hypnotic'' drugs. Sedatives can be used to produce an overly-calming effect ( alcohol being the m ...
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Anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and an innate response of the body to the environmental stimuli. Mild to moderate anxiety would increase level of performance. However, when anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses such as defensive behaviors, high levels of alertness and negative emotions, without external stimuli which induce anxiety within an individual. Those with anxiety disorders are also often found to have concurrent psychological disorders, most commonly depression. Anxiety disorders are divided into 6 types in clinical recognition. They are ...
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Designer Drug
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 ...
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Flubromazepam
Flubromazepam is a benzodiazepine derivative which was first synthesized in 1960, but was never marketed and did not receive any further attention or study until late 2012 when it appeared on the grey market as a novel designer drug. It is a structural analog of phenazepam in which the chlorine atom has been replaced by a fluorine atom. An alternate isomer, 5-(2-bromophenyl)-7-fluoro-1,3-dihydro-2''H''-1,4-benzodiazepin-2-one or "iso-flubromazepam", may have been sold under the same name. Legal status United Kingdom In the UK, flubromazepam 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. United States Flubromazepam, clonazolam, and flubromazolam are Schedule I controlled substances under Virginia State Law. See also * List of benzodiazepine designer drugs The below tables contain a sample list of benzodiazepines and benzodiazepine Analog (chemistry), anal ...
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Fludiazepam
Fludiazepam, marketed under the brand name Erispan (エリスパン) is a potent benzodiazepine and 2ʹ-fluoro derivative of diazepam, originally developed by Hoffman-La Roche in the 1960s. It is marketed in Japan and Taiwan. It exerts its pharmacological properties via enhancement of GABAergic inhibition. Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam. It possesses anxiolytic, anticonvulsant, sedative, hypnotic and skeletal muscle relaxant properties. Fludiazepam has been used recreationally. See also * Diazepam * Diclazepam (the 2ʹ-chloro analog) * Difludiazepam (the 2',6'-difluoro derivative) * Flunitrazepam (the 7-nitro analog) * Flualprazolam Flualprazolam is a tranquilizer of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. It was first synthesised in 1976, but was never marketed. It can be seen as the triazolo version of fludia ... (the triazolo derivative) * Ro ...
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Flutemazepam
Flutemazepam, initially first synthesized in 1965, but wasn't further developed and described until a team at Stabilimenti Chimici Farmaceutici Riuniti SpA in the mid 1970s. It is the fluorinated analogue of temazepam that has powerful hypnotic, sedative, amnesiac, anxiolytic, anticonvulsant and skeletal muscle relaxant properties. It is most closely related in structure to temazepam, being the fluoro instead of chloro analogue. As a result, flutemazepam has been shown to have similar pharmacological properties to temazepam and nimetazepam. It has been found to be effective for the treatment of the most severe states of anxiety, panic attacks, and severe insomnia. Furthermore, it is highly potent with 1 mg of flutemazepam being equivalent to 10 mg of diazepam. Flutemazepam is highly effective for acute psychotic states, especially stimulant psychosis, violent behaviour, and aggression. It was first synthesized and described in 1965 by Leo Sternbach. In a test which compared a ...
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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 ...
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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. ...
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