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Z-drug
Nonbenzodiazepines (), sometimes referred to colloquially as Z-drugs (as many of their names begin with the letter "z"), are a class of psychoactive drugs that are very benzodiazepine-like in nature. They are used in the treatment of sleep problems, and for their anxiolytic effects. Nonbenzodiazepine pharmacodynamics are almost entirely the same as benzodiazepine drugs and therefore exhibit similar benefits, side-effects, and risks. However, nonbenzodiazepines have dissimilar or entirely different chemical structures and are therefore unrelated to benzodiazepines on a molecular level. Classes Currently, the major chemical classes of nonbenzodiazepines are: Imidazopyridines * Alpidem * Necopidem * Saripidem * Zolpidem (Ambien, Ambien CR, Intermezzo, Zolpimist, Edluar, Ivadal, Sanval, Stilnox, etc.) Pyrazolopyrimidines * Divaplon * Fasiplon * Indiplon * Lorediplon * Ocinaplon * Panadiplon * Taniplon * Zaleplon (Sonata, Starnoc, Andante) Cyclopyrrolones * Eszopiclone (Lunesta ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eszopiclone
Eszopiclone, sold under the brand-name Lunesta among others such as Night Calm in Egypt, is a medication used in the treatment of insomnia. Evidence supports slight to moderate benefit up to six months. It is taken orally. Common side effects include headache, dry mouth, nausea, and dizziness. Severe side effects may include suicidal thoughts, unhealthy non-medical use, hallucinations, and angioedema. Greater care is recommended in those with liver problems and older people. Rapid decreasing of the dose may result in withdrawal. Eszopiclone is classified as a nonbenzodiazepine sedative hypnotic and as a cyclopyrrolone. It is the S-stereoisomer of zopiclone. It works by interacting with the GABA receptors. Approved for medical use in the United States in 2004, eszopiclone is available as generic medication. In 2020, it was the 232nd most commonly prescribed medication in the United States, with more than 1million prescriptions. Eszopiclone is not sold in the European Union, as o ... [...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 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 in conventional tablets, sublingual tablets, or oral spray. Common side effects include daytime sleepiness, headache, nausea, and diarrhea. More severe side effects include memory problems and hallucinations. The previously recommended dose was decreased in 2013, by the US Food and Drug Administration (FDA), to the immediate-release 10mg for men, and 5mg for women, in an attempt to reduce next-day somnolence. Newer extended-release formulations include the 6.25mg for women, and 12.5mg or 6.25mg for men, which also cause next-day somnolenc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ocinaplon
Ocinaplon is an anxiolytic drug in the pyrazolopyrimidine family of drugs. Other pyrazolopyrimidine drugs include zaleplon and indiplon. Ocinaplon has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and relatively little sedative or amnestic effect. Medical uses A 2019 review found tentative evidence of benefit in anxiety. Mechanism of action The mechanism of action by which ocinaplon produces its anxiolytic effects is by modulating GABAA receptors, although ocinaplon is more subtype-selective than most benzodiazepines. Availability Development of ocinaplon is discontinued due to liver complications that occurred in one of the Phase III subjects. Synthesis Condensation of 4-Acetylpyridine with N,N-Dimethylformamide dimethyl acetal ( DMFDMA) gives the "enamide" (3). This is then condensed with (3-Amino-1H-pyrazol-4-yl)(2-pyridinyl)methanone (4) (96219-90-8). This is the same intermediate as was used in the synthe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gedocarnil
Gedocarnil (INN) is an anxiolytic of the β-carboline class related to abecarnil. It is registered as an anxiolytic under the WHO's ATC classification system; however, there are no trade names associated with it and it does not appear to have ever been marketed. See also * Nonbenzodiazepine Nonbenzodiazepines (), sometimes referred to colloquially as Z-drugs (as many of their names begin with the letter "z"), are a class of psychoactive drugs that are very benzodiazepine-like in nature. They are used in the treatment of sleep proble ... References Anxiolytics Beta-Carbolines Chloroarenes Carboxylate esters Ethers Phenol ethers GABAA receptor positive allosteric modulators {{Anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abecarnil
Abecarnil (ZK-112,119) is an anxiolytic drug from the β-Carboline family. It is one of a relatively recently developed class of medicines known as the nonbenzodiazepines, which have similar effects to the older benzodiazepine group, but with quite different chemical structures. It is a partial agonist acting selectively at the benzodiazepine site of the GABAA receptor. Abecarnil was originally developed as an anti-anxiety drug, but has not as yet been commercially developed for use in humans, instead so far mainly being used for research into the development of other new sedative and anxiolytic drugs. Investigations are continuing into its actions and it looks likely to be developed for use both in the treatment of anxiety, and as a less addictive substitute drug for the treatment of benzodiazepine and alcohol addiction. Abecarnil may also have fewer problems of tolerance and withdrawal problems compared to nonselective full agonist benzodiazepine acting drugs. Abecarnil is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
β-Carboline
β-Carboline (9''H''- pyrido ,4-''b'' ndole) represents the basic chemical structure for more than one hundred alkaloids and synthetic compounds. The effects of these substances depend on their respective substituent. Natural β-carbolines primarily influence brain functions but can also exhibit antioxidant effects. Synthetically designed β-carboline derivatives have recently been shown to have neuroprotective, cognitive enhancing and anti-cancer properties. Pharmacology The pharmacological effects of specific β-carbolines are dependent on their substituents. For example, the natural β-carboline harmine has substituents on position 7 and 1. Thereby, it acts as a selective inhibitor of the DYRK1A protein kinase, a molecule necessary for neurodevelopment. It also exhibits various antidepressant-like effects in rats by interacting with serotonin receptor 2A. Furthermore, it increases levels of the brain-derived neurotrophic factor (BDNF) in rat hippocampus. A decreased BDNF le ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zopiclone
Zopiclone, sold under the brand name Imovane among others, is a nonbenzodiazepine used to treat insomnia, difficulty sleeping. Zopiclone is molecularly distinct from benzodiazepine drugs and is classed as a cyclopyrrolone. However, zopiclone increases the normal transmission of the neurotransmitter gamma-aminobutyric acid (GABA) in the central nervous system, via modulating GABAA receptor, GABAA receptors similarly to the way benzodiazepine drugs do. Zopiclone is a sedative. It works by causing a depression or tranquilization of the central nervous system. After prolonged use, the body can become accustomed to the effects of zopiclone. When the dose is then reduced or the drug is abruptly stopped, withdrawal symptoms may result. These can include a range of symptoms similar to those of benzodiazepine withdrawal. Although withdrawal symptoms from therapeutic doses of zopiclone and its isomers (i.e., eszopiclone) do not typically present with convulsions and are therefore not cons ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Suriclone
Suriclone (Suril) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Other cyclopyrrolone drugs include zopiclone and pagoclone. Suriclone has a very similar pharmacological profile to the benzodiazepine family of drugs including sedative and anxiolytic properties but with less amnestic effects, and its chemical structure A chemical structure determination includes a chemist's specifying the molecular geometry and, when feasible and necessary, the electronic structure of the target molecule or other solid. Molecular geometry refers to the spatial arrangement of at ... is quite different from that of the benzodiazepine drugs. The mechanism of action by which suriclone produces its sedative and anxiolytic effects is by modulating GABAA receptors, although suriclone is more subtype-selective than most benzodiazepines. References {{GABAAR PAMs Carbamates Chloroarenes Cyclopyrrolones GABAA receptor positive allosteric modulators Naphthyridines Pip ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Suproclone
Suproclone is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs, developed by the French pharmaceutical company Rhône-Poulenc. Other cyclopyrrolone drugs include zopiclone, pagoclone and suriclone. Suproclone is very similar in structure to the related drug suriclone Suriclone (Suril) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Other cyclopyrrolone drugs include zopiclone and pagoclone. Suriclone has a very similar pharmacological profile to the benzodiazepine family of drugs inc ..., but little information has been published about it specifically. However it can be expected that the mechanism of action by which suproclone produces its sedative and anxiolytic effects is by modulating benzodiazepine receptors (resulting in an increased response to endogenous GABA), in a similar manner to other drugs of this class. References Carbamates Chloroarenes Cyclopyrrolones GABAA receptor positive allosteric modulators Lactams ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pazinaclone
Pazinaclone (DN-2327) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Some other cyclopyrrolone drugs include zopiclone and eszopiclone. Pazinaclone has a very similar pharmacological profile to the benzodiazepines including sedative and anxiolytic properties, but with less amnestic effects, and at low doses it is a relatively selective anxiolytic, with sedative effects only appearing at higher doses. Pazinaclone produces its sedative and anxiolytic effects by acting as a partial agonist at GABAA benzodiazepine receptors, although pazinaclone is more subtype-selective than most benzodiazepines. Synthesis Reaction of 2-amino-7-chloro-1,8-naphthyridine with phthalic anhydride leads to the corresponding phthalimide. Selective reduction of one of the imide carbonyl groups in essence converts that to an aldehyde. Condensation with ''tert''-butyl(triphenylphosphoranylidene)acetate gives the Wittig product. The carboxylic acid is then treated with diethyl cy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pagoclone
Pagoclone is an anxiolytic agent from the cyclopyrrolone family, related to better-known drugs such as the sleeping medication zopiclone. It was synthesized by a French team working for Rhone-Poulenc & Rorer S.A. Pagoclone belongs to the class of nonbenzodiazepines, which have similar effects to the older benzodiazepine group, but with quite different chemical structures. It was never commercialised. It binds with roughly equivalent high affinity (0.7–9.1 nM) to the benzodiazepine binding site of human GABAA receptors containing either an α1, α2, α3 or α5 subunit. It is a partial agonist at α1-, α2- and α5-containing GABAA receptors and a full agonist at receptors containing an α3 subunit. In rats 5′-hydroxypagoclone was identified as a major metabolite. This metabolite has a considerably greater efficacy at the α1 subtype than the parent compound and was shown to have significant anxiolytic-like activity and to produce sedation. In contrast to zopiclone, pagoclone p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclopyrrolone
Cyclopyrrolones are a family of hypnotic and anxiolytic nonbenzodiazepine drugs with similar pharmacological profiles to the benzodiazepine derivatives. Although cyclopyrrolones are chemically unrelated to benzodiazepines, they function via the benzodiazepine receptor of neurotransmitter GABA. The best-known cyclopyrrolone derivatives are zopiclone (Imovane) and its active single-enantiomer component, eszopiclone (Lunesta), which are used to treat insomnia, and have a known potential for abuse. Other cyclopyrrolones include: * Pagoclone – anxiolytic * Pazinaclone – anxiolytic * Suproclone – anxiolytic * Suriclone Suriclone (Suril) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Other cyclopyrrolone drugs include zopiclone and pagoclone. Suriclone has a very similar pharmacological profile to the benzodiazepine family of drugs inc ... – anxiolytic References Chemical classes of psychoactive drugs {{heterocyclic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
