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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 Phthalic anhydride is the organic compound with the formula C6H4(CO)2O. It is the anhydride of phthalic acid. Phthalic anhydride is a principal commercial form of phthalic acid. It was the first anhydride of a dicarboxylic acid to be used commer ... leads to the corresponding ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pazinaclone Synthesis
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 Phthalic anhydride is the organic compound with the formula C6H4(CO)2O. It is the anhydride of phthalic acid. Phthalic anhydride is a principal commercial form of phthalic acid. It was the first anhydride of a dicarboxylic acid to be used commer ... leads to the corresponding p ... [...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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naphthyridine
Diazanaphthalenes are a class of aromaticity, aromatic heterocyclic compound, heterocyclic chemical compounds that have the formula C8H6N2. They consist of a naphthalene double ring in which two of the carbon atoms have been replaced with nitrogen atoms. There are ten positional isomers, which differ by the locations of the nitrogen atoms. The group consist of two subgroups: *four ''benzodiazines'' with both N atoms in one ring: cinnoline, quinazoline, quinoxaline, and phthalazine *six ''naphthyridines'' with one N atom in each ring Isomers References {{reflist Diazanaphthalenes, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acetamides
Acetamide (systematic name: ethanamide) is an organic compound with the formula CH3CONH2. It is an amide derived from ammonia and acetic acid. It finds some use as a plasticizer and as an industrial solvent. The related compound ''N'',''N''-dimethylacetamide (DMA) is more widely used, but it is not prepared from acetamide. Acetamide can be considered an intermediate between acetone, which has two methyl (CH3) groups either side of the carbonyl (CO), and urea which has two amide (NH2) groups in those locations. Acetamide is also a naturally occurring mineral with the IMA symbol: Ace. Production Laboratory scale Acetamide can be produced in the laboratory from ammonium acetate by dehydration: : H4CH3CO2] → CH3C(O)NH2 + H2O Alternatively acetamide can be obtained in excellent yield via ammonolysis of acetylacetone under conditions commonly used in reductive amination. It can also be made from anhydrous acetic acid, acetonitrile and very well dried hydrogen chloride gas, u ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lactams
A lactam is a cyclic amide, formally derived from an amino alkanoic acid through cyclization reactions. The term is a portmanteau of the words '' lactone'' + ''amide''. Nomenclature Greek prefixes in alphabetical order indicate ring size. This ring-size nomenclature stems from the fact that hydrolysis of an α-lactam gives an α-amino acid and that of a β-Lactam gives a β-amino acid, and so on. Synthesis General synthetic methods are used for the organic synthesis of lactams. Beckmann rearrangement Lactams form by the acid-catalyzed rearrangement of oximes in the Beckmann rearrangement. Schmidt reaction Lactams form from cyclic ketones and hydrazoic acid in the Schmidt reaction. Cyclohexanone with hydrazoic acid, forms ε - Caprolactum, which upon treatment with excess acid forms Cardiazole, a heart stimulant. Cyclization of amino acids Lactams can be formed from cyclisation of amino acids via the coupling between an amine and a carboxylic acid within the s ... [...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 central nervous system (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). Most sedatives 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. Terminology There is some overlap between the terms "sedative" and "hypnotic". Advances in pharmacol ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclopyrrolones
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 GABAA receptor, benzodiazepine receptor of neurotransmitter Gamma-aminobutyric acid, GABA. The best-known cyclopyrrolone derivatives are zopiclone (Imovane) and its enantiopure drug, 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 – anxiolytic References Cyclopyrrolones, Chemical classes of psychoactive drugs {{heterocyclic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phthalic Anhydride
Phthalic anhydride is the organic compound with the formula C6H4(CO)2O. It is the anhydride of phthalic acid. Phthalic anhydride is a principal commercial form of phthalic acid. It was the first anhydride of a dicarboxylic acid to be used commercially. This white solid is an important industrial chemical, especially for the large-scale production of plasticizers for plastics. In 2000, the worldwide production volume was estimated to be about 3 million tonnes per year. Synthesis and production Phthalic anhydride was first reported in 1836 by Auguste Laurent. Early procedures involved liquid-phase mercury-catalyzed oxidation of naphthalene. The modern industrial variant process instead uses vanadium pentoxide (V2O5) as the catalyst in a gas-phase reaction with naphthalene using molecular oxygen. The overall process involves oxidative cleavage of one of the rings and loss of two of the carbon atoms as carbon dioxide. An alternative process involves oxidation of the two m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 deceleration. Various kinds of sedatives can be distinguished, but the majority of them affect the neurotransmitter Gamma-Aminobutyric acid, gamma-aminobutyric acid (GABA). Most sedatives produce relaxing effects by increasing GABA activity. This group is related to hypnotics. The term ''sedative'' describes drugs that serve to calm or Anxiolytic, 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. Terminology There is some overlap ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiolytic
An anxiolytic (; also antipanic or anti-anxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and response. When anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses, such as defensive behaviors, high levels of alertness, and negative emotions. Those with anxiety disorders may have concurrent psychological disorders, such as depression. Anxiety disorders are classified using six possible clinical assessments: Different types of anxiety disorders will share some general symptoms while having their own distinctive symptoms. This explains why people with different types of anxiety disorders will respond differently to diffe ... [...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] |
