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Quinazolinone
Quinazolinone is a heterocyclic chemical compound, a quinazoline with a carbonyl group in the C4N2 ring. Two isomers are possible: 2-quinazolinone and 4-quinazolinone, with the 4-isomer being the more common. These compounds are of interest in medicinal chemistry. File:2-Quinazolinone.png, 2-Quinazolinone File:4-Quinazolinone.png, 4-Quinazolinone Synthesis Common routes to quinazolines involve condensation of amides to anilines with ortho nitrile, carboxylic acids and amides. Derivatives Quinazolinone drugs that function as hypnotic/sedative A sedative or tranquilliser is a substance that induces sedation by reducing irritability or Psychomotor agitation, excitement. They are central nervous system (CNS) Depressant, depressants and interact with brain activity, causing its decelera ...s, methaqualone (Quaalude) for example, usually contain a 4-quinazolinone core with a 2-substituted phenyl group at nitrogen atom 3. See also * Idelalisib (Zydelig) * Cloroqualone * S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Etaqualone
Etaqualone (Aolan, Athinazone, Ethinazone) is a quinazolinone-class GABAergic and is an analogue of methaqualone that was developed in the 1960s. It was primarily marketed in France and other European countries, as well as later in China, where it is still used clinically as of 2022. It has sedative, hypnotic, muscle relaxant and central nervous system depressant properties resulting from its agonist activity at the β-subtype of the GABAA receptor, and was used for the treatment of insomnia. The dosage and effects are reported to be similar to those of methaqualone, but shorter acting and slightly weaker. Typical reports use between 50 and 500 mg of etaqualone, depending on desired effects. Old pharmaceutical formulations of Ethinazone were 350 mg tablets. Etaqualone is thought to act in a similar way to barbiturates and benzodiazepines by increasing the sensitivity of GABAA receptors . Recreational effects include euphoria, relaxation, increased sociability and sex ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hypnotic
A hypnotic (from Ancient Greek, Greek ''Hypnos'', sleep), also known as a somnifacient or soporific, and commonly known as sleeping pills, are a class of psychoactive drugs whose primary function is to sleep induction, induce sleep and to treat insomnia (sleeplessness). This group of drugs is related to sedatives''. ''Whereas the term sedative describes drugs that serve to calm or Anxiolytic, relieve anxiety, the term hypnotic generally describes drugs whose main purpose is to initiate, sustain, or lengthen sleep. Because these two functions frequently overlap, and because drugs in this class generally produce dose-dependent effects (ranging from anxiolysis to loss of consciousness), they are often referred to collectively as sedative–hypnotic drugs. Hypnotic drugs are regularly prescribed for insomnia and other sleep disorders, with over 95% of insomnia patients being prescribed hypnotics in some countries. Many hypnotic drugs are habit-forming and—due to many factors kno ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methaqualone
Methaqualone is a hypnotic sedative. It was sold under the brand names Quaalude ( ) and Sopor among others, which contained 300 mg of methaqualone, and sold as a combination drug under the brand name Mandrax, which contained 250 mg methaqualone and 25 mg diphenhydramine within the same tablet, mostly in Europe. Commercial production of methaqualone was halted in the mid-1980s due to widespread abuse and addictiveness. It is a member of the quinazolinone class. Medical use The sedative–hypnotic activity of methaqualone was recognized in 1955. Its use peaked in the early 1970s for the treatment of insomnia, and as a sedative and muscle relaxant. Methaqualone was not recommended for use while pregnant and is in pregnancy category D. Similar to other GABAergic agents, methaqualone will produce tolerance and physical dependence with extended periods of use. Overdose An overdose of methaqualone can lead to coma and death. Additional effects are delirium, con ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diproqualone
Diproqualone is a quinazolinone class GABAergic and is an analogue of methaqualone developed in the late 1950s by a team at Nogentaise de Produits Chimique. It was marketed primarily in France and some other European countries. It has sedative, anxiolytic, antihistamine and analgesic properties, resulting from its agonist activity at the β subtype of the GABAa receptor, antagonist activity at all histamine receptors, inhibition of the cyclooxygenase-1 enzyme, and possibly its agonist activity at both the sigma-1 receptor and sigma-2 receptor (the function of these receptors and their clinical relevance has not yet been determined). Diproqualone is used primarily for treating inflammatory pain associated with osteoarthritis and rheumatoid arthritis and more rarely, for treating insomnia, anxiety and neuralgia. Diproqualone is the only analogue of methaqualone that is still in widespread clinical use, due to its useful anti-inflammatory and analgesic effects in addition to the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cloroqualone
Cloroqualone is a quinazolinone-class GABAergic and is an analogue of methaqualone developed in the 1980s and marketed mainly in France and some other European countries. It has sedative and antitussive properties resulting from its agonist activity at the β subtype of the GABAa receptor and sigma-1 receptor, and was sold either alone or in combination with other ingredients as a cough medicine. Cloroqualone has weaker sedative properties than methaqualone and was sold for its useful cough-suppressing effects, but was withdrawn from the French market in 1994 because of concerns about its potential for abuse and overdose. See also * Afloqualone * Etaqualone * Methylmethaqualone * Mecloqualone * Mebroqualone * Diproqualone * Gamma-Aminobutyric acid GABA (gamma-aminobutyric acid, γ-aminobutyric acid) is the chief inhibitory neurotransmitter in the developmentally mature mammalian central nervous system. Its principal role is reducing neuronal excitability throughout th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitromethaqualone
Nitromethaqualone is an analogue of methaqualone that has similar sedative and hypnotic A hypnotic (from Ancient Greek, Greek ''Hypnos'', sleep), also known as a somnifacient or soporific, and commonly known as sleeping pills, are a class of psychoactive drugs whose primary function is to sleep induction, induce sleep and to trea ... properties. It is significantly more potent (10×) compared to the parent compound; the typical dose is approximately 25 mg. References Sedatives Quinazolinones GABAA receptor positive allosteric modulators {{sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SL-164
SL-164, also known as dicloqualone or DCQ, is an analogue of methaqualone developed in the late 1960s by a team at Sumitomo. SL-164 has similar sedative, hypnotic and properties to the parent compound, but was never marketed for clinical use, due to higher risk of convulsions. Like other 4-substituted analogues, such as methylmethaqualone Methylmethaqualone (MMQ) is a quinazolinone and an analogue of methaqualone that has similar sedative and hypnotic properties to its parent compound (resulting from its agonist activity at the β subtype of the GABAA receptor) and is around 3 ti ..., SL-164 may cause seizures. References Sedatives Quinazolinones GABAA receptor positive allosteric modulators {{sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methylmethaqualone
Methylmethaqualone (MMQ) is a quinazolinone and an analogue of methaqualone that has similar sedative and hypnotic properties to its parent compound (resulting from its agonist activity at the β subtype of the GABAA receptor) and is around 3 times as potent in animal models. Methylmethaqualone differs from methaqualone by 4-methylation on the phenyl ring. It was made illegal in Germany in 1999 and listed by the DEA as a "drug of forensic interest" at about the same time, but little other information is available. It would appear that this compound was sold on the black market in Germany as a designer drug A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. ... analogue of methaqualone. Animal studies of methylmethaqualone have shown it to produce convulsions at only slightly above ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mecloqualone
Mecloqualone (Nubarene, Casfen) is a quinazolinone-class GABAergic and is an analogue of methaqualone that was first made in 1960 and marketed mainly in France and some other European countries. It has sedative, hypnotic, and anxiolytic properties caused by its agonist activity at the β subtype of the GABAa receptor, and was used for the treatment of insomnia. Mecloqualone is faster-acting but shorter-lasting than methaqualone and so was used only as a sleeping pill, in contrast to methaqualone, which was used as a general-purpose anxiolytic as well. Mecloqualone was never as widely used as methaqualone and is no longer prescribed because of concerns about its potential for abuse and overdose. In the United States it is a Schedule I non-narcotic (depressant) controlled substance with an ACSCN of 2572 and 30 grams annual aggregate manufacturing quota. See also * Afloqualone * Etaqualone * Methylmethaqualone * Mebroqualone * Cloroqualone * Diproqualone * Gamma-Aminobu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mebroqualone
Mebroqualone (MBQ) is a quinazolinone-class GABAergic and is an analogue of mecloqualone that has similar sedative and hypnotic properties to its parent compound, resulting from its agonist activity at the β subtype of the GABAa receptor. It was originally synthesized in the 1960s Mebroqualone differs from mecloqualone by having a bromine atom instead of a chlorine on the 3-phenyl ring. It was made illegal in Germany in 1998 but little other information is available. It would appear that this compound was sold on the black market in Germany as a designer drug analogue of mecloqualone. See also * Methaqualone * Afloqualone * Etaqualone * Methoxyqualone * Methylmethaqualone * Mecloqualone * Cloroqualone * Diproqualone * Gamma-Aminobutyric acid GABA (gamma-aminobutyric acid, γ-aminobutyric acid) is the chief inhibitory neurotransmitter in the developmentally mature mammalian central nervous system. Its principal role is reducing neuronal excitability throughout the ner ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinazoline
Quinazoline is an organic compound with the formula C8H6N2. It is an aromatic heterocycle with a bicyclic structure consisting of two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring. It is a light yellow crystalline solid that is soluble in water. Also known as 1,3-diazanaphthalene, quinazoline received its name from being an aza derivative of quinoline. Though the parent quinazoline molecule is rarely mentioned by itself in technical literature, substituted derivatives have been synthesized for medicinal purposes such as antimalarial and anticancer agents. Quinazoline is a planar molecule. It is isomeric with the other diazanaphthalenes of the benzodiazine subgroup: cinnoline, quinoxaline, and phthalazine. Over 200 biologically active quinazoline and quinoline alkaloids are identified. Synthesis : The synthesis of quinazoline was first reported in 1895 by August Bischler and Lang through the decarboxylation of the 2-carboxy derivative (quina ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Idelalisib
Idelalisib, sold under the brand name Zydelig, is a medication used to treat certain blood cancers. Idelalisib acts as a phosphoinositide 3-kinase inhibitor; more specifically, it blocks P110δ, the delta isoform of the enzyme phosphoinositide 3-kinase. It was developed by Gilead Sciences. It is taken orally (swallowed by mouth). Medical uses Idelalisib is a second-line medication for people whose chronic lymphocytic leukemia (CLL) has relapsed. Used in combination with rituximab, idelalisib is to be used in people for whom rituximab alone would be considered appropriate therapy due to other existing medical conditions. It appears to be effective and leads to improvement of lymphadenopathy and splenomegaly. However, the lymphocyte counts take longer to decrease to normal levels with idelalisib. It is not recommended as a first-line treatment. Adverse effects Clinical symptoms include diarrhea, fever, fatigue, nausea, cough, pneumonia, abdominal pain, chills and rash. Laborat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
