Deschloroetizolam
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Deschloroetizolam
Deschloroetizolam (also known as Etizolam-2) is a thienotriazolodiazepine that is the dechlorinated analog of the closely related etizolam. The compound has been sold as a designer drug. Legal status Deschloroetizolam is classified and controlled as a hazardous substance in Sweden as of on October 15, 2015. See also * Adinazolam * Clonazolam * Deschloroclotizolam * Diclazepam * Etizolam * Flubromazepam * Flubromazolam * Fluetizolam * Meclonazepam * Metizolam * Nifoxipam * Pyrazolam Pyrazolam (SH-I-04) is a benzodiazepine derivative originally developed by a team led by Leo Sternbach at Hoffman-La Roche in the 1970s. It has since been "rediscovered" and sold as a designer drug since 2012. Pyrazolam has structural similar ... References Designer drugs GABAA receptor positive allosteric modulators Hypnotics Thienotriazolodiazepines {{sedative-stub ...
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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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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 The etizolam molecule differs from a benzodiazepine in that the benzene ring has been replaced by a thiophene ring and triazole ring has been fused, making the drug a thienotriazolodiazepine.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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Deschloroclotizolam
Deschloroclotizolam is a thienotriazolodiazepine derivative which has been sold as a designer drug, first being identified in Sweden in 2021. See also * Alprazolam * Clotizolam * Fluclotizolam * Deschloroetizolam Deschloroetizolam (also known as Etizolam-2) is a thienotriazolodiazepine that is the dechlorinated analog of the closely related etizolam. The compound has been sold as a designer drug. Legal status Deschloroetizolam is classified and contro ... References Designer drugs GABAA receptor positive allosteric modulators Thienotriazolodiazepines Chloroarenes Phenyl compounds {{psychoactive-stub ...
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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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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 ...
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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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Pyrazolam
Pyrazolam (SH-I-04) is a benzodiazepine derivative originally developed by a team led by Leo Sternbach at Hoffman-La Roche in the 1970s. It has since been "rediscovered" and sold as a designer drug since 2012. Pyrazolam has structural similarities to alprazolam and bromazepam. Unlike other benzodiazepines, pyrazolam does not appear to undergo metabolism, instead being excreted unchanged in the urine. It is most selective for the α2 and α3 subtypes of the GABAA receptor, GABAA receptor. Legal Status United Kingdom In the UK, pyrazolam has been classified as a Drugs controlled by the UK Misuse of Drugs Act, Class C drug by section 5 of the May 2017 amendment to Misuse of Drugs Act 1971, The Misuse of Drugs Act 1971 along with several other designer benzodiazepine drugs. See also * List of benzodiazepine designer drugs References

{{GABAAR PAMs Triazolobenzodiazepines GABAA receptor positive allosteric modulators Designer drugs 2-Pyridyl compo ...
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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 ...
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Metizolam
Metizolam (also known as desmethyletizolam) is a thienotriazolodiazepine that is the demethylated analogue of the closely related etizolam. Legal status Following its sale as a designer drug, metizolam was classified as controlled substance in Sweden on 26. January 2016. See also * 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 Chloroarenes Designer drugs GABAA receptor positive allosteric modulators Hypnotics Thienotriazolodiazepines {{sedative-stub ...
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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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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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