|
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clotiazepam
Clotiazepam (marketed under brand name Clozan, Distensan, Trecalmo, Rize, Rizen and Veratran) is a thienodiazepine drug which is a benzodiazepine analog. The clotiazepam molecule differs from benzodiazepines in that the benzene ring has been replaced by a thiophene ring. It possesses anxiolytic, skeletal muscle relaxant, anticonvulsant, sedative properties. Stage 2 NREM sleep is significantly increased by clotiazepam. Indications Clotiazepam has been trialed and found to be effective in the short-term management of anxiety. Clotiazepam is also used as a premedicant in minor surgery in France and Japan, where the drug is commercially available under the brand names ''Veratran'' and ''Rize'', respectively. Pharmacokinetics A cross-over study in six healthy volunteers (median age 28 years) was conducted using single-dose pharmacokinetics of 5 mg clotiazepam drops, oral tablets, and sublingual tablets. The formulations had similar systemic availability. Compared with ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clotizolam
Clotizolam (Ro11-1465) is a thienotriazolodiazepine derivative first invented in the 1970s, which in more recent years has been sold as a designer drug. As with other related thienotriazolodiazepines, it produces sedative, anxiolytic, anticonvulsant and muscle relaxant effects, and also acts as an inhibitor of platelet-activating factor (PAF). See also * Brotizolam * Etizolam * Flubrotizolam * Fluclotizolam * Deschloroclotizolam * 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 ... * Triazolam References Designer drugs GABAA receptor positive allosteric modulators Thienotriazolodiazepines Chloroarenes Phenyl compounds {{psychoactive-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diclazepam
Diclazepam (Ro5-3448), also known as chlorodiazepam and 2'-chloro-diazepam, is a benzodiazepine and functional analog of diazepam. It was first synthesized by Leo Sternbach and his team at Hoffman-La Roche in 1960. It is not currently approved for use as a medication, but rather sold as an unscheduled substance. Efficacy and safety have not been tested in humans. In animal models, its effects are similar to diazepam, possessing long-acting anxiolytic, anticonvulsant, hypnotic, sedative, skeletal muscle relaxant, and amnestic properties. Metabolism Metabolism of this compound has been assessed, revealing diclazepam has an approximate elimination half-life of 42 hours and undergoes ''N''-demethylation to delorazepam, which can be detected in urine for 6 days following administration of the parent compound. Other metabolites detected were lorazepam and lormetazepam which were detectable in urine for 19 and 11 days, respectively, indicating hydroxylation by cytochrome P450 enzyme ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thienodiazepine
A thienodiazepine is a heterocyclic compound containing a diazepine ring fused to a thiophene Thiophene is a heterocyclic compound with the formula C4H4S. Consisting of a planar five-membered ring, it is aromatic as indicated by its extensive substitution reactions. It is a colorless liquid with a benzene-like odor. In most of its react ... ring. :If R1 and R2 are part of a triazole ring, the substance is called a " thienotriazolodiazepine." The thienodiazepine structure forms the central core of some pharmaceutical and recreational drugs, including: * Bentazepam * Clotiazepam * Etizolam * Metizolam * Deschloroetizolam Since thienodiazepines interact with the benzodiazepine receptor site, they typically have similar effects as benzodiazepines. References Thienodiazepines {{heterocyclic-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] |
Ro20-8552
Ro20-8552 is a benzodiazepine derivative with sedative and anxiolytic effects, which has been sold as a designer drug. See also * Ro05-2904 * Ro05-4435 * 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 struct ... * Ro07-4065 * Ro20-8065 References Designer drugs GABAA receptor positive allosteric modulators Benzodiazepines Fluoroarenes Chloroarenes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ro07-4065
Difludiazepam (Ro07-4065) is a benzodiazepine derivative which is the 2',6'-difluoro derivative of fludiazepam. It was invented in the 1970s but was never marketed, and has been used as a research tool to help determine the shape and function of the GABAA receptors, at which it has an IC50 of 4.1nM. Difludiazepam has subsequently been sold as a designer drug, and was first notified to the EMCDDA by Swedish authorities in 2017. See also * Diclazepam * Flubromazepam * Ro07-5220 * 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 ... References {{GABAAR PAMs Benzodiazepines Fluoroarenes GABAA receptor positive allosteric modulators ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
