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Idazoxan Synthesis
Idazoxan (International Nonproprietary Name, INN) is a drug which is used in scientific research. It acts as both a selective alpha-2 receptor, α2 adrenergic receptor Receptor antagonist, antagonist, and an antagonist for the imidazoline receptor. Idazoxan has been under investigation as an antidepressant, but it did not reach the market as such. More recently, it is under investigation as an adjunctive treatment in schizophrenia. Due to its alpha-2 receptor antagonism it is capable of enhancing therapeutic effects of antipsychotics, possibly by enhancing dopamine neurotransmission in the prefrontal cortex of the brain, a brain area thought to be involved in the pathogenesis of schizophrenia. Alzheimer's research Mice treated with idazoxan, which blocks the Alpha-2A adrenergic receptor, α2A receptor which regulates norepinephrine, behaved similarly to control animals despite still having amyloid-beta plaques in the brain, as a proof-of-concept experiment that dramatically red ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Racemic Mixture
In chemistry, a racemic mixture, or racemate (), is one that has equal amounts of left- and right-handed enantiomers of a chiral molecule or salt. Racemic mixtures are rare in nature, but many compounds are produced industrially as racemates. History The first known racemic mixture was racemic acid, which Louis Pasteur found to be a mixture of the two enantiomeric isomers of tartaric acid. He manually separated the crystals of a mixture by hand, starting from an aqueous solution of the sodium ammonium salt of racemate tartaric acid. Pasteur benefited from the fact that ammonium tartrate salt that gives enantiomeric crystals with distinct crystal forms (at 77 °F). Reasoning from the macroscopic scale down to the molecular, he reckoned that the molecules had to have non-superimposable mirror images. A sample with only a single enantiomer is an ''enantiomerically pure'' or ''enantiopure'' compound. Etymology From racemic acid found in grapes; from Latin ''racemus'', meani ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pathogenesis
Pathogenesis is the process by which a disease or disorder develops. It can include factors which contribute not only to the onset of the disease or disorder, but also to its progression and maintenance. The word comes from Greek πάθος ''pathos'' 'suffering, disease' and γένεσις ''genesis'' 'creation'. Description Types of pathogenesis include microbial infection, inflammation, malignancy and tissue breakdown. For example, bacterial pathogenesis is the process by which bacteria cause infectious illness. Most diseases are caused by multiple processes. For example, certain cancers arise from dysfunction of the immune system (skin tumors and lymphoma after a renal transplant, which requires immunosuppression), Streptococcus pneumoniae is spread through contact with respiratory secretions, such as saliva, mucus, or cough droplets from an infected person and colonizes the upper respiratory tract and begins to multiply. The pathogenic mechanisms of a disease (or cond ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Imidazoline Antagonists
Imidazoline is a class of heterocycles formally derived from imidazoles by the reduction of one of the two double bonds. Three isomers are known, 2-imidazolines, 3-imidazolines, and 4-imidazolines. The 2- and 3-imidazolines contain an imine In organic chemistry, an imine ( or ) is a functional group or organic compound containing a carbon–nitrogen double bond (). The nitrogen atom can be attached to a hydrogen or an organic group (R). The carbon atom has two additional single bo ... center, whereas the 4-imidazolines contain an alkene group. The 2-Imidazoline group occurs in several drugs.Liu, H. and Du, D.-M. (2009), Recent Advances in the Synthesis of 2-Imidazolines and Their Applications in Homogeneous Catalysis. Adv. Synth. Catal., 351: 489–519. doi: 10.1002/adsc.200800797 References Imidazolines, {{Organic-chemistry-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha Blockers
Alpha (uppercase , lowercase ; grc, ἄλφα, ''álpha'', or ell, άλφα, álfa) is the first letter of the Greek alphabet. In the system of Greek numerals, it has a value of one. Alpha is derived from the Phoenician letter aleph , which is the West Semitic word for " ox". Letters that arose from alpha include the Latin letter A and the Cyrillic letter А. Uses Greek In Ancient Greek, alpha was pronounced and could be either phonemically long ( ː or short ( . Where there is ambiguity, long and short alpha are sometimes written with a macron and breve today: Ᾱᾱ, Ᾰᾰ. * ὥρα = ὥρᾱ ''hōrā'' "a time" * γλῶσσα = γλῶσσᾰ ''glôssa'' "tongue" In Modern Greek, vowel length has been lost, and all instances of alpha simply represent the open front unrounded vowel . In the polytonic orthography of Greek, alpha, like other vowel letters, can occur with several diacritic marks: any of three accent symbols (), and either of two breathing marks ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluparoxan
Fluparoxan (developmental code name GR50360A) is a potent α2-adrenergic receptor antagonist (pKB = 7.9) with excellent selectivity for this receptor over the α1-adrenergic receptor (2,630-fold), and is the only well-studied α2-adrenergic receptor antagonist in its structural family which does not antagonize any variant of the imidazoline receptor. It was shown to possess central α2-adrenoceptor antagonist activity after oral doses in man and was patented as an antidepressant by Glaxo in the early 1980s, but its development was discontinued when the compound failed to show a clear clinical advantage over existing therapies. Pharmacology Pharmacodynamics Fluparoxan is a very selective α2-adrenergic blocker, that readily crosses the blood–brain barrier. Blockade of α2-adrenoreceptors, particularly presynaptic autoreceptors in noradrenergic neurons by fluparoxan, produces an increase in the synaptic concentrations of noradrenaline, by blocking the autoinhibitory feedback me ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Efaroxan
Efaroxan is an α2-adrenergic receptor antagonist and antagonist of the imidazoline receptor. Synthesis The Darzens reaction between 2-fluorobenzaldehyde 7848-46-1(1) and Ethyl 2-bromobutyrate 33-68-6(2) gives ethyl 2-ethyl-3-(2-fluorophenyl)oxirane-2-carboxylateCID:100942311(3). A catalytic hydrogenation over Pd/C would give ethyl 2- 2-fluorophenyl)methyl2-hydroxybutanoateCID:77591056(4). Saponification of the ester then gives 2- 2-Fluorophenyl)methyl2-hydroxybutanoic acidCID:53869347(5). Treatment with 2 molar equivalents of sodium hydride apparently gives 2-Ethyl-2,3-dihydrobenzofuran-2-carboxylic acid 11080-50-3(6). Treatment of the carboxylic acid with thionyl chloride then gives the acid chloride and subsequent treatment of this with ethylenediamine in the presence of trimethylaluminium completed the synthesis of ' (8). See also * Fluparoxan * Idazoxan Idazoxan (INN) is a drug which is used in scientific research. It acts as both a selective α2 adrenergic receptor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Imiloxan
Imiloxan is a drug which is used in scientific research. It acts as a selective Receptor antagonist, antagonist for the Alpha-2B adrenergic receptor, α2B adrenergic receptor, and has been useful for distinguishing the actions of the different α2 adrenergic subtypes. Synthesis The imidazole portion of imiloxan is prepared by the reaction of an imidate with the diethyl acetal of aminoacetaldehyde. ''N''-Alkylation of the imidazole with ethyl iodide gives imiloxan. References External links * Imidazolines Alpha blockers Benzodioxans {{antihypertensive-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ethylenediamine
Ethylenediamine (abbreviated as en when a ligand) is the organic compound with the formula C2H4(NH2)2. This colorless liquid with an ammonia-like odor is a basic amine. It is a widely used building block in chemical synthesis, with approximately 500,000 tonnes produced in 1998.Karsten Eller, Erhard Henkes, Roland Rossbacher, Hartmut Höke "Amines, Aliphatic" in Ullmann's Encyclopedia of Industrial Chemistry, 2005 Wiley-VCH Verlag, Weinheim. Ethylenediamine is the first member of the so-called polyethylene amines. Synthesis Ethylenediamine is produced industrially by treating 1,2-dichloroethane with ammonia under pressure at 180 °C in an aqueous medium:Hans-Jürgen Arpe, Industrielle Organische Chemie, 6. Auflage (2007), Seite 245, Wiley VCH : In this reaction hydrogen chloride is generated, which forms a salt with the amine. The amine is liberated by addition of sodium hydroxide and can then be recovered by . Diethylenetriamine (DETA) and triethylenetetramine (TETA) a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pinner Reaction
The Pinner reaction refers to the acid catalysed reaction of a nitrile with an alcohol to form an imino ester salt (alkyl imidate salt); this is sometimes referred to as a Pinner salt. The reaction is named after Adolf Pinner, who first described it in 1877. Pinner salts are themselves reactive and undergo additional nucleophilic additions to give various useful products: * With an excess of alcohol to form an orthoester * With ammonia or an amine to form an amidine (di-nitriles may form imidines, for instance succinimidine from succinonitrile) * With water to form an ester * With hydrogen sulfide to form a thionoester Commonly the Pinner salt itself is not isolated, with the reaction being continued to give the desired functional group (orthoester etc.) in one go. It should be appreciated that the Pinner reaction refers specifically to an acid catalyzed process, but that similar results can often be achieved using base catalysis. The two approaches can be complementary, with ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Idazoxan Synthesis
Idazoxan (International Nonproprietary Name, INN) is a drug which is used in scientific research. It acts as both a selective alpha-2 receptor, α2 adrenergic receptor Receptor antagonist, antagonist, and an antagonist for the imidazoline receptor. Idazoxan has been under investigation as an antidepressant, but it did not reach the market as such. More recently, it is under investigation as an adjunctive treatment in schizophrenia. Due to its alpha-2 receptor antagonism it is capable of enhancing therapeutic effects of antipsychotics, possibly by enhancing dopamine neurotransmission in the prefrontal cortex of the brain, a brain area thought to be involved in the pathogenesis of schizophrenia. Alzheimer's research Mice treated with idazoxan, which blocks the Alpha-2A adrenergic receptor, α2A receptor which regulates norepinephrine, behaved similarly to control animals despite still having amyloid-beta plaques in the brain, as a proof-of-concept experiment that dramatically red ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alzheimer's Disease
Alzheimer's disease (AD) is a neurodegeneration, neurodegenerative disease that usually starts slowly and progressively worsens. It is the cause of 60–70% of cases of dementia. The most common early symptom is difficulty in short-term memory, remembering recent events. As the disease advances, symptoms can include primary progressive aphasia, problems with language, Orientation (mental), disorientation (including easily getting lost), mood swings, loss of motivation, self-neglect, and challenging behaviour, behavioral issues. As a person's condition declines, they often withdraw from family and society. Gradually, bodily functions are lost, ultimately leading to death. Although the speed of progression can vary, the typical life expectancy following diagnosis is three to nine years. The cause of Alzheimer's disease is poorly understood. There are many environmental and genetic risk factors associated with its development. The strongest genetic risk factor is from an alle ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norepinephrine
Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad'', "near", and '' ren'', "kidney") is more commonly used in the United Kingdom, whereas "norepinephrine" (from Ancient Greek ἐπῐ́ (''epí''), "upon", and νεφρός (''nephrós''), "kidney") is usually preferred in the United States. "Norepinephrine" is also the international nonproprietary name given to the drug. Regardless of which name is used for the substance itself, parts of the body that produce or are affected by it are referred to as noradrenergic. The general function of norepinephrine is to mobilize the brain and body for action. Norepinephrine release is lowest during sleep, rises during wakefulness, and reaches much higher levels during situations of stress or danger, in the so-called fight-or-flight response. In the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enantiomer_and_(-)Enantiomer.svg "Click for more on -> Fluparoxan")
