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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 the treatment of 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 ... [...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] |
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. Quinazolinone drugs that function as hypnotic/sedatives usually contain a 4-quinazolinone core with a 2-substituted phenyl group at nitrogen atom 3. See also * Idelalisib (Zydelig) * Methaqualone (Quaalude) * Cloroqualone * SL-164 (Dicloqualone) * Diproqualone * Etaqualone * Mebroqualone * Mecloqualone * Methylmethaqualone * Nitromethaqualone Nitromethaqualone is an analogue of methaqualone Methaqualone is a hypnotic sedative. It was sold under the brand names Quaalude ( ) and Sopor among others, wh ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Afloqualone
Afloqualone (Arofuto) is a quinazolinone family GABAergic drug and is an analogue of methaqualone developed in the 1970s by a team at Tanabe Seiyaku. It has sedative and muscle-relaxant effects resulting from its agonist activity at the β subtype of the GABAa receptor and has had some clinical use, although it causes photosensitization as a side-effect that can cause skin problems such as dermatitis. See also * Methaqualone * Diproqualone * Etaqualone * Methylmethaqualone * Mecloqualone * Mebroqualone * Cloroqualone * Nitromethaqualone Nitromethaqualone is an analogue of 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 th ... References Sedatives Muscle relaxants Organofluorides Quinazolinones GABAA receptor positive allosteric modulators {{sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinazolinones
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. Quinazolinone drugs that function as hypnotic/sedatives usually contain a 4-quinazolinone core with a 2-substituted phenyl group at nitrogen atom 3. See also * Idelalisib (Zydelig) * Methaqualone (Quaalude) * Cloroqualone * SL-164 (Dicloqualone) * Diproqualone * Etaqualone * Mebroqualone * Mecloqualone * Methylmethaqualone * Nitromethaqualone Nitromethaqualone is an analogue of methaqualone Methaqualone is a hypnotic sedative. It was sold under the brand names Quaalude ( ) and Sopor among others, wh ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diols
A diol is a chemical compound containing two hydroxyl groups ( groups). An aliphatic diol is also called a glycol. This pairing of functional groups is pervasive, and many subcategories have been identified. The most common industrial diol is ethylene glycol. Examples of diols in which the hydroxyl functional groups are more widely separated include 1,4-butanediol and propylene-1,3-diol, or beta propylene glycol, . Synthesis of classes of diols Geminal diols A geminal diol has two hydroxyl groups bonded to the same atom. These species arise by hydration of the carbonyl compounds. The hydration is usually unfavorable, but a notable exception is formaldehyde which, in water, exists in equilibrium with methanediol H2C(OH)2. Another example is (F3C)2C(OH)2, the hydrated form of hexafluoroacetone. Many gem-diols undergo further condensation to give dimeric and oligomeric derivatives. This reaction applies to glyoxal and related aldehydes. Vicinal diols In a vicinal diol, t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesics
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing to t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sedatives
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are CNS depressants and interact with brain activity causing its deceleration. Various kinds of sedatives can be distinguished, but the majority of them affect the neurotransmitter gamma-aminobutyric acid (GABA). In spite of the fact that each sedative acts in its own way, most produce relaxing effects by increasing GABA activity. This group is related to hypnotics. The term ''sedative'' describes drugs that serve to calm or relieve anxiety, whereas the term ''hypnotic'' 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. Sedatives can be used to produce an overly-calming effect (alcohol being the most ... [...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 * Methaqualone * Afloqualone * Etaqualone * Methylmethaqualone * Mecloqualone * Mebroqualone * 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 sed ... [...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 * Methylmethaqualone * Mecloqualone * Cloroqualone * 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 ... * Gamma-Aminobutyric acid ... [...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 g annual aggregate manufacturing quota. See also * Methaqualone * Afloqualone * Etaqualone * Methylmethaqualone * Mebroqualone * Cloroqualone * Diproqualone Diproqual ... [...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 much more potent. 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 analogue of methaqualone. Animal studies of methylmethaqualone have shown it to produce convulsions A convulsion is a medical condition where the body muscles contract and relax rapidly and repeatedly, resulting in uncontrolled shaking. Because epileptic seizures typically include convulsions, the term ''convulsion'' is sometimes used as a s ... at only slightly above the effective sedative do ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
