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Fluetizolam
Fluetizolam (2-ethyl-4-(2-fluorophenyl)-9-methyl-6H-thieno,2-f1,2,4]triazolo ,3-a1,4]diazepine) is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects, which has been sold as a designer drug. See also * Brotizolam * Clotiazepam * Flualprazolam * Flubrotizolam * Fluclotizolam * Etizolam * Ro09-9212 Ro09-9212 is a thienodiazepine derivative with sedative and anxiolytic effects, which has been sold as a designer drug. See also * Clotiazepam * Clotizolam * Diclazepam * Etizolam * Flubrotizolam * Fluclotizolam Fluclotizolam is a thieno ... References Designer drugs GABAA receptor positive allosteric modulators Heterocyclic compounds with 3 rings Diazepines Triazoles Sulfur heterocycles Fluoroarenes {{sedative-stub ...
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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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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 The etizolam molecule differs from a benzodiazepine in that the benzene ring has been replaced by a thiophene ring and triazole ring has been fused, making the drug a thienotriazolodiazepine.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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Ro09-9212
Ro09-9212 is a thienodiazepine derivative with sedative and anxiolytic effects, which has been sold as a designer drug. See also * Clotiazepam * Clotizolam * Diclazepam * Etizolam * Flubrotizolam * 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 ... * Fluetizolam * Ro07-4065 * Ro20-8552 References Designer drugs GABAA receptor positive allosteric modulators Diazepines Chlorobenzenes Thiophenes {{sedative-stub ...
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Triazoles
A triazole is a heterocyclic compound featuring a five-membered ring of two carbon atoms and three nitrogen atoms with molecular formula C2H3N3. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. Many triazoles are versatile, biologically active compounds commonly used as fungicides and plant retardants. However, triazoles are also useful in bioorthogonal chemistry, because the large number of nitrogen atoms causes triazoles to react similar to azides. Lastly, the many free lone pairs in triazoles make them useful as coordination compounds, although not typically as haptic ligands. Isomerism There are four triazole isomers, which are conventionally divided into two pairs of tautomers. In the 1,2,3-triazoles, the three nitrogen atoms are adjacent; in the 1,2,4-triazoles, an interstitial carbon separates out one nitrogen atom. Each category has two tautomers that differ by which nitrogen has a hydrogen bonded ...
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Heterocyclic Compounds With 3 Rings
A heterocyclic compound or ring structure is a cyclic compound that has atoms of at least two different elements as members of its ring(s). Heterocyclic chemistry is the branch of organic chemistry dealing with the synthesis, properties, and applications of these heterocycles. Examples of heterocyclic compounds include all of the nucleic acids, the majority of drugs, most biomass (cellulose and related materials), and many natural and synthetic dyes. More than half of known compounds are heterocycles. 59% of US FDA-approved drugs contain nitrogen heterocycles. Classification The study of heterocyclic chemistry focuses especially on unsaturated derivatives, and the preponderance of work and applications involves unstrained 5- and 6-membered rings. Included are pyridine, thiophene, pyrrole, and furan. Another large class of heterocycles refers to those fused to benzene rings. For example, the fused benzene derivatives of pyridine, thiophene, pyrrole, and furan are quinol ...
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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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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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Thienotriazolodiazepine
A thienotriazolodiazepine is a heterocyclic compound containing a diazepine ring fused to thiophene and triazole rings. Thienotriazolodiazepine forms the central core of several pharmaceutical drugs including: * Brotizolam * Ciclotizolam * Deschloroetizolam * Etizolam * Fluclotizolam * Metizolam Thienotriazolodiazepines interact with the benzodiazepine receptor site, they typically have similar effects as 1,4- benzodiazepines (such as diazepam) and triazolobenzodiazepines (such as alprazolam Alprazolam, sold under the brand name Xanax, among others, is a fast-acting, potent tranquilizer of medium duration in the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. It is most commonly u ...). Thienotriazolodiazepines that are not GABAA receptor positive allosteric modulators include: * Israpafant * JQ1 References {{heterocyclic-stub ...
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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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Flubrotizolam
Flubrotizolam (2-bromo-4-(2-fluorophenyl)-9-methyl-6H-thieno,2-f1,2,4]triazolo ,3-a1,4]diazepine) is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects, which has been sold as a designer drug. See also * Brotizolam * Deschloroclotizolam * Flubromazolam * Fluclotizolam * 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 ha ... References Designer drugs GABAA receptor positive allosteric modulators Heterocyclic compounds with 3 rings Nitrogen heterocycles Sulfur heterocycles Bromoarenes Fluoroarenes {{sedative-stub ...
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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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