Flualprazolam
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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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Etizolam
Etizolam (marketed under many brand names) is a thienodiazepine derivative which is a benzodiazepine analog. The etizolam molecule differs from a benzodiazepine in that the benzene ring has been replaced by a thiophene ring and triazole ring has been fused, making the drug a thienotriazolodiazepine. Although a thienodiazepine, etizolam is clinically regarded as a benzodiazepine because of its mode of action via the benzodiazepine receptor and directly targeting GABAA receptors. It possesses anxiolytic, amnesic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. Etizolam is an anxiolytic found to have lower tolerance and dependence liability than benzodiazepines. It was patented in 1972 and approved for medical use in 1983. As of April 2021, the export of Etizolam has been banned in India. Medical uses * Short-term treatment of insomnia. * Anxiety disorders such as OCD and general anxiety disorder, mostly as a short-term medication to be used pur ...
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Flubromazolam
Flubromazolam (JYI-73) is a triazolobenzodiazepine (TBZD), which are benzodiazepine (BZD) derivatives. Flubromazolam is reputed to be highly potent, and concerns have been raised that clonazolam and flubromazolam in particular may pose comparatively higher risks than other designer benzodiazepines, due to their ability to produce strong sedation and amnesia at oral doses of as little as 0.5 mg. Life-threatening adverse reactions have been observed at doses of only 3 mg of flubromazolam. Legal status Sweden Flubromazolam has been classified as an illegal substance in Sweden after seizures by customs and police, as well as indications from the EMCDDA of wider use as a recreational drug. Switzerland Flubromazolam is illegal in Switzerland as of December 2015. United Kingdom In the UK, flubromazolam 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. Australia I ...
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Triazolobenzodiazepines
upChemical structure of alprazolam, a common triazolobenzodiazepine Triazolobenzodiazepines (TBZD) are a class of benzodiazepine (BZD) derivative pharmaceutical drugs. Chemically, they differ from other benzodiazepines by having an additional fused triazole ring. Examples include: * Adinazolam * Alprazolam * Bromazolam * Clonazolam * Estazolam * Flualprazolam * Flubromazolam * Flunitrazolam * Nitrazolam * Pyrazolam * Triazolam Triazolam, sold under the brand name Halcion among others, is a central nervous system (CNS) depressant tranquilizer of the triazolobenzodiazepine (TBZD) class, which are benzodiazepine (BZD) derivatives. It possesses pharmacological properties ... * Zapizolam Synthesis Synthesis of 1-methyltriazolobenzodiazepines (alprazolam type) is possible by heating 1,4-benzodiazepin-2- thiones with hydrazine and acetic acid in ''n''-butanol under reflux.Hester JB, Duchamp DJ, Chidester CG (1971): "A synthetic approach to new 1,4-benzodiazepine derivatives." Tetr ...
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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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Clonazolam
Clonazolam (also known as clonitrazolam) is a drug of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. It has had very little research done about its effects and metabolism, and has been sold online as a designer drug. The synthesis of clonazolam was first reported in 1971 and the drug was described as the most active compound in the series tested. Clonazolam is reported to be highly potent and concerns have been raised that it and flubromazolam in particular may pose comparatively higher risk than other designer benzodiazepines due to their ability to produce strong sedation and amnesia at as little as 0.5 mg. Legality United Kingdom In the UK, clonazolam 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 It is a Schedule I medicine in Virginia, Louisiana, North Carolina and Oregon and is not FDA ap ...
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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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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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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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Triazolobenzodiazepine
upChemical structure of alprazolam, a common triazolobenzodiazepine Triazolobenzodiazepines (TBZD) are a class of benzodiazepine (BZD) derivative pharmaceutical drugs. Chemically, they differ from other benzodiazepines by having an additional fused triazole ring. Examples include: * Adinazolam * Alprazolam * Bromazolam * Clonazolam * Estazolam * Flualprazolam * Flubromazolam * Flunitrazolam * Nitrazolam * Pyrazolam * Triazolam Triazolam, sold under the brand name Halcion among others, is a central nervous system (CNS) depressant tranquilizer of the triazolobenzodiazepine (TBZD) class, which are benzodiazepine (BZD) derivatives. It possesses pharmacological properties ... * Zapizolam Synthesis Synthesis of 1-methyltriazolobenzodiazepines (alprazolam type) is possible by heating 1,4-benzodiazepin-2- thiones with hydrazine and acetic acid in ''n''-butanol under reflux.Hester JB, Duchamp DJ, Chidester CG (1971): "A synthetic approach to new 1,4-benzodiazepine derivatives." Tetr ...
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Fluorine
Fluorine is a chemical element with the symbol F and atomic number 9. It is the lightest halogen and exists at standard conditions as a highly toxic, pale yellow diatomic gas. As the most electronegative reactive element, it is extremely reactive, as it reacts with all other elements except for the light inert gases. Among the elements, fluorine ranks 24th in universal abundance and 13th in terrestrial abundance. Fluorite, the primary mineral source of fluorine which gave the element its name, was first described in 1529; as it was added to metal ores to lower their melting points for smelting, the Latin verb meaning 'flow' gave the mineral its name. Proposed as an element in 1810, fluorine proved difficult and dangerous to separate from its compounds, and several early experimenters died or sustained injuries from their attempts. Only in 1886 did French chemist Henri Moissan isolate elemental fluorine using low-temperature electrolysis, a process still employed for modern pr ...
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Flurazepam
Flurazepam (marketed under the brand names Dalmane and Dalmadorm) is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. It produces a metabolite with a long half-life, which may stay in the bloodstream for days. Flurazepam was patented in 1968 and came into medical use the same year. Flurazepam, developed by Roche Pharmaceuticals was one of the first benzo hypnotics (sleeping pills) to be marketed. Medical uses Flurazepam is officially indicated for mild to moderate insomnia and as such it is used for short-term treatment of patients with mild to moderate insomnia such as difficulty falling asleep, frequent awakening, early awakenings or a combination of each. Flurazepam is a long-acting benzodiazepine and is sometimes used in patients who have difficulty in maintaining sleep, though benzodiazepines with intermediate half-lives such as loprazolam, lormetazepam, and temazepam ...
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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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