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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 a binding affinity of 0.77nM at the α1 subtype, 0.17nM at α2, 0.38nM at α3 and 0.11nM at α5. It has been used to study the functional differences between the different subtypes of the GABAA receptor. See also * GL-II-73 * QH-II-66 QH-II-66 (QH-ii-066) is a sedative drug which is a benzodiazepine derivative. It produces some of the same effects as other benzodiazepines, but is much more selective than most other drugs of this class and so produces somewhat less sedation a ... * SH-053-R-CH3-2'F References {{GABAAR PAMs Benzodiazepines GABAA receptor positive allosteric modulators ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 It is a structural analog of phenazepam in which the chlorine atom has been replaced by a fluorine atom.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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GL-II-73
GL-II-73 (GL-ii-073) is a benzodiazepine derivative related in chemical structure to compounds such as midazolam and adinazolam. It is described as an α5 preferring positive allosteric modulator of the benzodiazepine site of GABAA receptors, with weaker activity at α2 and α3 and no significant affinity for the α1 subtype. In animal tests it was found to produce effects consistent with antidepressant, anxiolytic and nootropic actions. See also * Imidazenil * QH-II-66 * SH-I-048A * SH-053-R-CH3-2'F * Ro4938581 Ro4938581 is a nootropic drug invented in 2009 by a team working for Hoffmann-La Roche, which acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor. It has good selectivity f ... References {{GABAAR PAMs GABAA receptor positive allosteric modulators Imidazobenzodiazepines Nootropics ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
QH-II-66
QH-II-66 (QH-ii-066) is a sedative drug which is a benzodiazepine derivative. It produces some of the same effects as other benzodiazepines, but is much more selective than most other drugs of this class and so produces somewhat less sedation and ataxia than other related drugs such as diazepam and triazolam, although it still retains anticonvulsant effects. QH-ii-066 is a highly subtype-selective GABAA agonist which was designed to bind selectively to the α5 subtype of GABAA receptors. The α5 subtype (and to a lesser extent the α1 subtype) of GABAA are two of the most important targets in the brain that produce the effects of alcohol, and so one of the purposes for which QH-ii-066 was developed was to reproduce the GABAergic effects of alcohol separately from its other actions. QH-ii-066 replicates some of the effects of alcohol, such as sedation and ataxia, but does not increase appetite, as this effect seems to be produced by the α1 subtype of GABAA rather than α ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzodiazepine
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, insomnia, and seizures. The first benzodiazepine, chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955 and was made available in 1960 by Hoffmann–La Roche, who soon followed with diazepam (Valium) in 1963. By 1977, benzodiazepines were the most prescribed medications globally; the introduction of selective serotonin reuptake inhibitors (SSRIs), among other factors, decreased rates of prescription, but they remain frequently used worldwide. Benzodiazepines are depressants that enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABAA receptor, resulting in sedative, hypnotic ( sleep-inducing), anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant properties. High doses o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Superagonist
In the field of pharmacology, a superagonist is a type of agonist that is capable of producing a maximal response greater than the endogenous agonist for the target receptor, and thus has an efficacy of more than 100%. For example, goserelin is a superagonist of the gonadotropin-releasing hormone receptor. See also * Agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ... References Receptor agonists {{Pharmacology-stub ... [...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] |
Affinity (pharmacology)
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 molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition of liga ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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, insomnia, and seizures. The first benzodiazepine, chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955 and was made available in 1960 by Hoffmann–La Roche, who soon followed with diazepam (Valium) in 1963. By 1977, benzodiazepines were the most prescribed medications globally; the introduction of selective serotonin reuptake inhibitors (SSRIs), among other factors, decreased rates of prescription, but they remain frequently used worldwide. Benzodiazepines are depressants that enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABAA receptor, resulting in sedative, hypnotic ( sleep-inducing), anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant properties. High doses of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
