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Pyrazolopyrimidines
Pyrazolopyrimidines are a series of isomeric heterocyclic chemical compounds with the molecular formula C6H5N3. They form the central core of a variety of more complex chemical compounds including some pharmaceuticals and pesticides. Pharmaceuticals One isomer of pyrazolopyrimidines, known as pyrazolo[1,5-''a'']pyrimidine, is the basis for a class of sedative and anxiolytic medication, drugs related (in terms of their effect) to benzodiazepines. Most of the drugs from this class marketed to date are intended to induce sleep, and are prescribed for people suffering insomnia, however some newer compounds produce anxiolytic effects with relatively little sedation, and are being developed for use as non-sedating anti-anxiety drugs. They include: * Zaleplon - hypnotic (trade name Sonata) * Indiplon - hypnotic * Ocinaplon - anxiolytic * Lorediplon - hypnotic As they are not chemically related to the benzodiazepines despite their similar effect, such drugs—as well as the imidazopy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zaleplon
Zaleplon, sold under the brand name Sonata among others, is a sedative and hypnotic which is used to treat insomnia. It is a nonbenzodiazepine or Z-drug of the pyrazolopyrimidine class. It was developed by King Pharmaceuticals and approved for medical use in the United States in 1999. Medical uses Zaleplon is slightly effective in treating insomnia, primarily characterized by difficulty falling asleep. Zaleplon significantly reduces the time required to fall asleep by improving sleep latency and may therefore facilitate sleep induction rather than sleep maintenance. Due to its ultrashort elimination half-life, zaleplon may not be effective in reducing premature awakenings; however, it may be administered to alleviate middle-of-the-night awakenings. However, zaleplon has not been empirically shown to increase total sleep time. Zaleplon does not significantly affect driving performance the morning following bedtime administration or 4 hours after middle-of-the-night administ ... [...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] |
Pyrazophos
Pyrazophos is an organic compound used as a fungicide and an insecticide. Uses Pyrazophos is a systemic fungicide which is used in orchards, vineyards and vegetable crops against powdery mildew. In some instances, the compound is also an effective insecticide Insecticides are pesticides used to kill insects. They include ovicides and larvicides used against insect eggs and larvae, respectively. The major use of insecticides is in agriculture, but they are also used in home and garden settings, i ... (e.g. against leaf-miner flies). History The compound has been commercially available since 1970. References External links * Pyrazolopyrimidines Fungicides Insecticides Ethyl esters Organophosphates {{alkanederivative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zaleplon Skeletal
Zaleplon, sold under the brand name Sonata among others, is a sedative and hypnotic which is used to treat insomnia. It is a nonbenzodiazepine or Z-drug of the pyrazolopyrimidine class. It was developed by King Pharmaceuticals and approved for medical use in the United States in 1999. Medical uses Zaleplon is slightly effective in treating insomnia, primarily characterized by difficulty falling asleep. Zaleplon significantly reduces the time required to fall asleep by improving sleep latency and may therefore facilitate sleep induction rather than sleep maintenance. Due to its ultrashort elimination half-life, zaleplon may not be effective in reducing premature awakenings; however, it may be administered to alleviate middle-of-the-night awakenings. However, zaleplon has not been empirically shown to increase total sleep time. Zaleplon does not significantly affect driving performance the morning following bedtime administration or 4 hours after middle-of-the-night administr ... [...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] |
Indiplon
Indiplon ( INN and USAN) is a unmarketed nonbenzodiazepine, hypnotic sedative that was developed in two formulations—an immediate-release formulation for sleep onset, and a modified-release (also called controlled-release or extended-release) version for sleep maintenance. Pharmacology Pharmacodynamics Indiplon works by enhancing the action of the inhibitory neurotransmitter GABA, like most other nonbenzodiazepine sedatives. It primarily binds to the α1 subunits of the GABAA receptors in the brain. Pharmacokinetics Indiplon has a short elimination half-life of 1.5 to 1.8 hours in young and elderly subjects, respectively. Chemistry Indiplon is a pyrazolopyramidine related to the nonbenzodiazepine hypnotic zaleplon. History Indiplon was discovered at Lederle Laboratories (which was later acquired by Wyeth) in the 1980s and was called CL 285,489. In 1998 Lederle licensed it, along with other early stage drug candidates, to DOV Pharmaceutical, a startup formed by ... [...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 synth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Insomnia
Insomnia, also known as sleeplessness, is a sleep disorder where people have difficulty sleeping. They may have difficulty falling asleep, or staying asleep for as long as desired. Insomnia is typically followed by daytime sleepiness, low energy, irritability, and a depression (mood), depressed mood. It may result in an increased risk of accidents of all kinds as well as problems focusing and learning. Insomnia can be short term, lasting for days or weeks, or long term, lasting more than a month. The concept of the word ''insomnia'' has two distinct possibilities: insomnia disorder (ID) or insomnia symptoms, and many abstracts of randomized controlled trials and systematic reviews often underreport on which of these two possibilities the word refers to. Insomnia can occur independently or as a result of another problem. Conditions that can result in insomnia include psychological stress, chronic pain, heart failure, hyperthyroidism, heartburn, restless leg syndrome, menopause ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sleep
Sleep is a state of reduced mental and physical activity in which consciousness is altered and certain Sensory nervous system, sensory activity is inhibited. During sleep, there is a marked decrease in muscle activity and interactions with the surrounding environment. While sleep differs from wakefulness in terms of the ability to react to Stimulus (physiology), stimuli, it still involves active Human brain, brain patterns, making it more reactive than a coma or disorders of consciousness. Sleep occurs in sleep cycle, repeating periods, during which the body alternates between two distinct modes: rapid eye movement sleep (REM) and Non-rapid eye movement sleep, non-REM sleep. Although REM stands for "rapid eye movement", this mode of sleep has many other aspects, including virtual Rapid eye movement sleep#Muscle, paralysis of the body. Dreams are a succession of images, ideas, emotions, and sensations that usually occur involuntarily in the mind during certain stages of sleep. ... [...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] |
Heterocyclic
A heterocyclic compound or ring structure is a cyclic compound that has atoms of at least two different elements as members of its ring(s). Heterocyclic organic chemistry is the branch of organic chemistry dealing with the synthesis, properties, and applications of organic heterocycles. Examples of heterocyclic compounds include all of the nucleic acids, the majority of drugs, most biomass (cellulose and related materials), and many natural and synthetic dyes. More than half of known compounds are heterocycles. 59% of US FDA-approved drugs contain nitrogen heterocycles. Classification The study of organic heterocyclic chemistry focuses especially on organic unsaturated derivatives, and the preponderance of work and applications involves unstrained organic 5- and 6-membered rings. Included are pyridine, thiophene, pyrrole, and furan. Another large class of organic heterocycles refers to those fused to benzene rings. For example, the fused benzene derivatives of p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
