|
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 The etizolam molecule differs from a benzodiazepine in that the benzene ring has been replaced by a thiophene ring and triazole ring has been fused, making the drug a thienotriazolodiazepine.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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thienotriazolodiazepines General Structure
Thienobenzodiazepine is a heterocyclic compound containing a diazepine ring fused to a thiophene ring and a benzene ring. Thienobenzodiazepine forms the central core of pharmaceutical drugs including atypical antipsychotic olanzapine (Zyprexa) and antimuscarinic telenzepine Telenzepine is a thienobenzodiazepine acting as selective M1 antimuscarinic. It is used in the treatment of peptic ulcers. Telenzepine is atropisomer Atropisomers are stereoisomers arising because of hindered rotation about a single bond, wh .... Thienobenzodiazepines act relatively selectively at the α2 subunit of the GABAA receptor. Thienobenzodiazepines {{heterocyclic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Brotizolam
Brotizolam (marketed under brand name Lendormin) is a sedative-hypnotic thienotriazolodiazepine drug which is a benzodiazepine analog. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties, and is considered to be similar in effect to other short-acting hypnotic benzodiazepines such as triazolam or midazolam. It is used in the short-term treatment of severe insomnia. Brotizolam is a highly potent and short-acting hypnotic, with a typical dose ranging from 0.125 to 0.25 milligrams, which is rapidly eliminated with an average half-life of 4.4 hours (range 3.6–7.9 hours). It was patented in 1974 and came into medical use in 1984. Brotizolam is not approved for sale in the UK, United States or Canada. It is approved for sale in the Netherlands, Germany, Spain, Belgium, Luxembourg, Austria, Portugal, Israel, Italy, Taiwan and Japan. Medical uses Brotizolam is prescribed for the short-term treatment, 2–4 weeks only of severe or debil ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ciclotizolam
CiclotizolamDE Patent 2445430 (WE-973) is a drug which is a thienotriazolodiazepine derivative. It is a partial agonist for the benzodiazepine site of the GABAA receptor, with similar binding affinity In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a m ... to related compounds like brotizolam, but a low efficacy. See also * Benzodiazepine References Chloroarenes GABAA receptor positive allosteric modulators Bromoarenes Thienotriazolodiazepines Cyclohexyl compounds {{sedative-stub ... [...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] |
Israpafant
Israpafant (Y-24180) is a drug which acts as a selective antagonist for the platelet-activating factor receptor, and was originally developed for the treatment of asthma. Its chemical structure is a thienotriazolodiazepine, closely related to the sedative benzodiazepine derivative etizolam. However israpafant binds far more tightly to the platelet-activating factor receptor, with an IC50 of 0.84nM for inhibiting PAF-induced human platelet aggregation (compared to etizolam's IC50 of 998nM at this target), while it binds only weakly to benzodiazepine receptors, with a Ki of 3680nM. Israpafant has been found to inhibit the activation of eosinophil cells, and consequently delays the development of immune responses. It has also been shown to have anti-nephrotoxic properties, and to mobilize calcium transport. See also * JQ1 JQ1 is a thienotriazolodiazepine and a potent inhibitor of the BET family of bromodomain proteins which include BRD2, BRD3, BRD4, and the testis-specific ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diazepine
Diazepine is a seven-membered heterocyclic compound with two nitrogen atoms (e.g., in ring positions 1 and 2). Types include: * 1,2-diazepine * 1,3-diazepine * 1,4-diazepine ** Benzodiazepines 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, i ..., a class of commonly used medications whose structure contains a 1,4-diazepine ring {{heterocyclic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 reactions, it resembles benzene. Compounds analogous to thiophene include furan (C4H4O), selenophene (C4H4Se) and pyrrole (C4H4NH), which each vary by the heteroatom in the ring. Isolation and occurrence Thiophene was discovered as a contaminant in benzene. It was observed that isatin (an indole) forms a blue dye if it is mixed with sulfuric acid and crude benzene. The formation of the blue indophenin had long been believed to be a reaction of benzene itself. Viktor Meyer was able to isolate thiophene as the actual substance responsible for this reaction. Thiophene and especially its derivatives occur in petroleum, sometimes in concentrations up to 1–3%. The thiophenic content of oil and coal is removed via the hydrodesulfurization (HDS) ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Triazole
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABAA Receptor
The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Upon opening, the GABAA receptor on the postsynaptic cell is selectively permeable to chloride ions (Cl−) and, to a lesser extent, bicarbonate ions (HCO3−). Depending on the membrane potential and the ionic concentration difference, this can result in ionic fluxes across the pore. If the membrane potential is higher than the equilibrium potential (also known as the reversal potential) for chloride ions, when the receptor is activated Cl− will flow into the cell. This causes an inhibitory effect on neurotransmission by diminishing the chance of a successful action potential occurring at the postsynaptic cell. The reversal potential of the GABAA-mediated inhibitory postsynaptic potential (IPSP) in normal solution is −70 mV, contrasting the GABAB IPSP (-100 mV). T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
