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DS-1 (drug)
DS-1 is a drug from the imidazopyridine family, which is the first drug developed that acts as a GABAA receptor positive allosteric modulator (PAM) selective for the α4 β3 δ subtype, which is not targeted by other GABAA receptor PAMs such as the benzodiazepines or other nonbenzodiazepine drugs. Novel selective drugs such as DS-1 are useful in the study of this receptor subtype. See also * Alpidem * Saripidem * Zolpidem Zolpidem, sold under the brand name Ambien among others, is a medication primarily used for the short-term treatment of sleeping problems. Guidelines recommend that it be used only after cognitive behavioral therapy for insomnia and after beh ... References Benzamides 4-Chlorophenyl compounds GABAA receptor positive allosteric modulators Imidazopyridines Bromoarenes Thiophenes {{sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Imidazopyridine
An imidazopyridine is a nitrogen containing heterocycle that is also a class of medication, drugs that contain this same chemical substructure. In general, they are GABAA receptor, GABAA receptor receptor_agonist, agonists, however recently proton pump inhibitors, aromatase inhibitors, NSAIDs and other classes of drugs in this class have been developed as well. Despite usually being similar to them in effect, they are not chemically related to benzodiazepines. As such, GABAA-agonizing imidazopyridines, pyrazolopyrimidines, and cyclopyrrones are sometimes grouped together and referred to as "nonbenzodiazepines." Imidazopyridines include: Sedatives Anxiolytics, sedatives and hypnotics (GABAA receptor positive allosteric modulator, GABAA receptor positive allosteric modulators): * Imidazo[1,2-a]pyridines: ** Alpidem (original brand name Ananxyl)—an anxiolytic that was withdrawn from the market worldwide in 1995 due to hepatotoxicity. ** DS-1 (drug), DS-1—a GABAA receptor, GABAA ... [...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 (biochemistry), ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Accurate regulation of GABAergic transmission through appropriate developmental processes, specificity to neural cell types, and responsiveness to activity is crucial for the proper functioning of nearly all aspects of the central nervous system (CNS). Upon opening, the GABAA receptor on the Chemical synapse, postsynaptic cell is selectively permeable to Chloride, chloride ions () and, to a lesser extent, Bicarbonate, bicarbonate ions (). GABAAR are members of the ligand-gated ion channel receptor superfamily, which is a chloride channel family with a dozen or more heterotetrametric subtypes and 19 distinct subunits. These subtypes have distinct brain regional and subcellular localization, age-dependent expression, and the ability to undergo plastic alt ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Positive Allosteric Modulator
In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimuli. Some of them, like benzodiazepines or alcohol, function as psychoactive drugs. The site that an allosteric modulator binds to (i.e., an ''allosteric site'') is not the same one to which an endogenous agonist of the receptor would bind (i.e., an ''orthosteric site''). Modulators and agonists can both be called receptor ligands. Allosteric modulators can be 1 of 3 types either: positive, negative or neutral. Positive types increase the response of the receptor by increasing the probability that an agonist will bind to a receptor (i.e. affinity), increasing its ability to activate the receptor (i.e. efficacy), or both. Negative types decrease the agonist affinity and/or efficacy. Neutral types don't affect agonist activity but can stop other modulators from binding to an allosteric site. Some modulators also work as allosteric agonis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABRA4
Gamma-aminobutyric acid receptor subunit alpha-4 is a protein that in humans is encoded by the ''GABRA4'' gene In biology, the word gene has two meanings. The Mendelian gene is a basic unit of heredity. The molecular gene is a sequence of nucleotides in DNA that is transcribed to produce a functional RNA. There are two types of molecular genes: protei .... GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated chloride channels. Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABA-A receptor. At least 16 distinct subunits of GABA-A receptors have been identified. A research study compared wild-type to knockout GABRA4 gene in mice. It was determined that the elimination of the GABRA4 gene displayed characteristics that are associated with autism spectrum disorder (ASD). These include increased spatial cognition and decreased social engagement, u ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABRB3
Gamma-aminobutyric acid receptor subunit beta-3 is a protein that in humans is encoded by the ''GABRB3'' gene. It is located within the 15q12 region in the human genome and spans 250kb. This gene includes 10 exons within its coding region. Due to alternative splicing, the gene codes for many protein isoforms, all being subunits in the GABAA receptor, a ligand-gated ion channel. The beta-3 subunit is expressed at different levels within the cerebral cortex, hippocampus, cerebellum, thalamus, olivary body and piriform cortex of the brain at different points of development and maturity. GABRB3 deficiencies are implicated in many human neurodevelopmental disorders and syndromes such as Angelman syndrome, Prader-Willi syndrome, nonsyndromic orofacial clefts, epilepsy and autism. The effects of methaqualone and etomidate are mediated through GABBR3 positive allosteric modulation. Gene The GABRB3 gene is located on the long arm of chromosome 15, within the q12 region in the human g ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABRD
Gamma-aminobutyric acid receptor subunit delta is a protein that in humans is encoded by the ''GABRD'' gene. In the mammalian brain, the delta (δ) subunit forms specific GABAA receptor subtypes by co-assembly leading to δ subunit containing GABAA receptors (δ-GABAA receptors). Function The delta (δ) subunit, one of the subunits of the hetero-pentameric δ-GABAA receptors, is a determinant subunit for the specific cellular localization of δ-GABAA receptors, which are modulated by the GABA. GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts on the repertoire of GABAA receptors, the ligand-gated chloride channels. It is assembled from a diverse subunit pool, including assemblies from a family of 19 subunits (α1-α6, β1-β3, γ1-γ3, δ, ∈, θ, π and ρ1-ρ3). The GABRD gene encodes the delta (δ) subunit. Specifically, the δ-subunit is usually expressed in GABAA receptors associated with extrasynaptic activity, mediating tonic inhibition ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzodiazepine
Benzodiazepines (BZD, BDZ, BZs), colloquially known as "benzos", are a class of central nervous system (CNS) depressant, 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 Roche, Hoffmann–La Roche, which followed with the development of diazepam (Valium) three years later, 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, gamma-aminobutyric acid (GABA) at the GABAA receptor, GABAA receptor, resulting ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nonbenzodiazepine
Nonbenzodiazepines (), sometimes referred to colloquially as Z-drugs (as many of their names begin with the letter "z"), are a class of psychoactive, depressant, sedative, hypnotic, anxiolytic drugs that are benzodiazepine-like in uses, such as for treating insomnia and anxiety. Nonbenzodiazepine pharmacodynamics are similar in mechanism of action to benzodiazepine drugs, acting as GABAA receptor positive allosteric modulator, GABAA receptor positive allosteric modulators of the benzodiazepine receptor, benzodiazepine site, and therefore exhibit similar benefits, side effects, and risks. However, nonbenzodiazepines have dissimilar or entirely different chemical structures, so are unrelated to benzodiazepines on a molecular level. Background Nonbenzodiazepines have demonstrated efficacy in treating sleep disorders. There is some limited evidence that suggests that drug tolerance, tolerance to nonbenzodiazepines is slower to develop than with benzodiazepines. However, data is limit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpidem
Alpidem, sold under the brand name Ananxyl, is a nonbenzodiazepine anxiolytic medication which was briefly used to treat anxiety disorders but is no longer marketed. It was previously marketed in France, but was list of withdrawn drugs, discontinued due to liver toxicity. Alpidem is taken oral administration, by mouth. Side effects of alpidem include sedation, fatigue (medical), fatigue, dizziness, and headache, among others. It has much less to no impact on cognition, memory, and Psychomotor agitation, psychomotor function relative to benzodiazepines. Similarly, no rebound effect, rebound anxiety or withdrawal symptoms have been observed with alpidem. Rarely, alpidem can cause serious liver toxicity, including liver failure and death. Alpidem is a nonbenzodiazepine of the imidazopyridine family, chemical structure, structurally related to the Z-drug zolpidem, and acts as a GABAA receptor positive allosteric modulator, GABAA receptor positive allosteric modulator of the benzodia ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Saripidem
Saripidem is a sedative and anxiolytic drug in the imidazopyridine family, which is related to the better known drugs zolpidem and alpidem. Saripidem has a similar pharmacological profile to the benzodiazepine family of drugs including sedative and anxiolytic properties, but its chemical structure is quite different from that of the benzodiazepine drugs, and saripidem is described as a nonbenzodiazepine. The mechanism of action by which saripidem produces its sedative and anxiolytic effects is by modulating the benzodiazepine binding site on GABAA receptors, however unlike many older GABAA agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...s, saripidem is highly subtype selective and binds primarily to the ω1 subtype. References {{GABAAR PAMs Carboxamides 4-Chl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zolpidem
Zolpidem, sold under the brand name Ambien among others, is a medication primarily used for the short-term treatment of sleeping problems. Guidelines recommend that it be used only after cognitive behavioral therapy for insomnia and after behavioral changes, such as sleep hygiene, have been tried. It decreases the time to sleep onset by about fifteen minutes and at larger doses helps people stay asleep longer. It is taken by mouth and is available as conventional tablets, extended-release tablets, or sublingual tablets. Common side effects include daytime sleepiness, headache, nausea, and diarrhea. More severe side effects include memory problems and hallucinations. While flumazenil, a GABAA receptor antagonist, can reverse zolpidem's effects, usually supportive care is all that is recommended in overdose. Zolpidem is a nonbenzodiazepine, or Z-drug, which acts as a sedative and hypnotic as a positive allosteric modulator at the GABAA receptor. It is an imidazopyrid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzamides
Benzamide is an organic compound with the chemical formula of C7H7NO. It is the simplest amide derivative of benzoic acid. In powdered form, it appears as a white solid, while in crystalline form, it appears as colourless crystals. It is slightly soluble in water, and soluble in many organic solvents. It is a natural alkaloid Alkaloids are a broad class of natural product, naturally occurring organic compounds that contain at least one nitrogen atom. Some synthetic compounds of similar structure may also be termed alkaloids. Alkaloids are produced by a large varie ... found in the herbs of '' Berberis pruinosa''. Chemical derivatives A number of substituted benzamides are commercial drugs, including: See also * References External links Physical characteristics {{Authority control Phenyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
