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Flopropione
Flopropione (Compacsul, Cospanon, Ecapron, Pellegal, Argobyl, Floveton, Saritron, Spamorin, Labrodax, Tryalon, Mirulevatin, Padeskin, Profenon) is a spasmolytic or antispasmodic agent. It acts as a COMT inhibitor. It is synthesized from phloroglucinol in a Hoesch reaction. See also *2,4,6-Trihydroxyacetophenone 2,4,6-Trihydroxyacetophenone (THAP) is a chemical compound that is a derivative of phloroglucinol. In an animal model, THAP was reported to enhance cholesterol 7 alpha-hydroxylase (CYP7A1) activity. THAP is also used as a matrix in matrix-assis ... (THAP) References Phloroglucinols Aromatic ketones Serotonin receptor antagonists 3-Hydroxypropenals {{musculoskeletal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Muscle Relaxant
A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therapeutic groups: Neuromuscular-blocking drugs, neuromuscular blockers and Antispasmodic, spasmolytics. Neuromuscular blockers act by interfering with transmission at the neuromuscular end plate and have no central nervous system (CNS) activity. They are often used during surgical procedures and in intensive care and emergency medicine to cause temporary paralysis. Spasmolytics, also known as "centrally acting" muscle relaxant, are used to alleviate musculoskeletal pain and spasms and to reduce spasticity in a variety of neurological conditions. While both neuromuscular blockers and spasmolytics are often grouped together as muscle relaxant, [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antispasmodic
An antispasmodic (synonym: spasmolytic) is a pharmaceutical drug or other agent that suppresses muscle spasms. Smooth muscle spasm One type of antispasmodics is used for smooth muscle relaxation, especially in tubular organs of the gastrointestinal tract. The effect is to prevent spasms of the stomach, intestine or urinary bladder. Both dicyclomine and hyoscyamine are antispasmodic due to their anticholinergic action. Both of these drugs have side effects common to anticholinergics and can worsen gastroesophageal reflux disease (GERD). Papaverine is an opium alkaloid used to treat visceral spasms, particularly those of the intestines. Mebeverine is a papaverine analog and spasmolytic with a strong and selective action on the smooth muscles of the gastrointestinal tract, particularly of the colon. Despite being anticholinergic, it does not have the systemic anticholinergic side effects seen in other such drugs. Peppermint oil has been traditionally used as an antispasmodic, and a r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
COMT
Catechol-''O''-methyltransferase (COMT; ) is one of several enzymes that degrade catecholamines (neurotransmitters such as dopamine, epinephrine, and norepinephrine), catecholestrogens, and various drugs and substances having a catechol structure. In humans, catechol-''O''-methyltransferase protein is encoded by the COMT gene. Two isoforms of COMT are produced: the soluble short form (S-COMT) and the membrane bound long form (MB-COMT). As the regulation of catecholamines is impaired in a number of medical conditions, several pharmaceutical drugs target COMT to alter its activity and therefore the availability of catecholamines. COMT was first discovered by the biochemist Julius Axelrod in 1957. Function Catechol-''O''-methyltransferase is involved in the inactivation of the catecholamine neurotransmitters (dopamine, epinephrine, and norepinephrine). The enzyme introduces a methyl group to the catecholamine, which is donated by S-adenosyl methionine (SAM). Any compound havin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Inhibitory Postsynaptic Potential
An inhibitory postsynaptic potential (IPSP) is a kind of synaptic potential that makes a postsynaptic neuron less likely to generate an action potential.Purves et al. Neuroscience. 4th ed. Sunderland (MA): Sinauer Associates, Incorporated; 2008. The opposite of an inhibitory postsynaptic potential is an excitatory postsynaptic potential (EPSP), which is a synaptic potential that makes a postsynaptic neuron ''more'' likely to generate an action potential. IPSPs can take place at all chemical synapses, which use the secretion of neurotransmitters to create cell-to-cell signalling. EPSPs and IPSPs compete with each other at numerous synapses of a neuron. This determines whether an action potential occurring at the presynaptic terminal produces an action potential at the postsynaptic membrane. Some common neurotransmitters involved in IPSPs are GABA and glycine. Inhibitory presynaptic neurons release neurotransmitters that then bind to the postsynaptic receptors; this induces a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phloroglucinol
Phloroglucinol is an organic compound with the formula C6H3(OH)3. It is a colorless solid. It is used in the organic synthesis, synthesis of pharmaceuticals and explosives. Phloroglucinol is one of three isomeric benzenetriols. The other two isomers are hydroxyquinol (1,2,4-benzenetriol) and pyrogallol (1,2,3-benzenetriol). Phloroglucinol, and its benzenetriol isomers, are still defined as "natural phenol, phenols" according to the IUPAC official nomenclature rules of chemical compounds. Many such monophenolics are often termed polyphenols. The enzyme is biosynthesized by phloroglucinol synthase. Synthesis and occurrence In 1855, phloroglucinol was first prepared from phloretin by the Austrian chemist Heinrich Hlasiwetz (1825–1875). A modern synthesis of phloroglucinol involves hydrolysis of benzene-1,3,5-triamine and its derivatives. Representative is the following route from 1,3,5-Trinitrobenzene, trinitrobenzene. : The synthesis is noteworthy because ordinary aniline deriv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hoesch Reaction
The Hoesch reaction or Houben–Hoesch reaction is an organic reaction in which a nitrile reacts with an arene compound to form an aryl ketone. The reaction is a type of Friedel–Crafts acylation with hydrogen chloride and a Lewis acid catalyst. The synthesis of 2,4,6-Trihydroxyacetophenone (THAP) from phloroglucinol is representative: If two-equivalents are added, 2,4-Diacetylphloroglucinol is the product. : An imine can be isolated as an intermediate reaction product. The attacking electrophile is possibly a species of the type R-C+=NHCl−. The arene must be electron-rich i.e. phenol or aniline type. A related reaction is the Gattermann reaction in which hydrocyanic acid not a nitrile is used. The reaction is named after Kurt Hoesch and Josef Houben''Über die Kern-Kondensation von Phenolen und Phenol-äthern mit Nitrilen zu Phenol- und Phenol-äther-Ketimiden und -Ketonen (I.)'' Berichte der deutschen chemischen Gesellschaft (A and B Series) Volume 59, Issue 11, Date: 8. De ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2,4,6-Trihydroxyacetophenone
2,4,6-Trihydroxyacetophenone (THAP) is a chemical compound that is a derivative of phloroglucinol. In an animal model, THAP was reported to enhance cholesterol 7 alpha-hydroxylase (CYP7A1) activity. THAP is also used as a matrix in matrix-assisted laser desorption/ionization (MALDI) for the analysis of acidic glycans and glycopeptides in negative ion mode. Derivatives THAP is a chemical precursor that can be used to form part of the backbone of 5,7-dihydroxyflavones like noreugenin, apigenin Apigenin (4′,5,7-trihydroxyflavone), found in many plants, is a flavone compound that is the aglycone of several naturally occurring glycosides. It is a yellow crystalline solid that has been used to dye wool. Apigenin is abundant in parsl ..., luteolin, diosmetin, naringenin, and hesperetin. See also * Flopropione References {{DEFAULTSORT:Trihydroxyacetophenone, 2,4,6- Phloroglucinols Aromatic ketones 3-Hydroxypropenals ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phloroglucinols
Phloroglucinol is an organic compound with the formula C6H3(OH)3. It is a colorless solid. It is used in the synthesis of pharmaceuticals and explosives. Phloroglucinol is one of three isomeric benzenetriols. The other two isomers are hydroxyquinol (1,2,4-benzenetriol) and pyrogallol (1,2,3-benzenetriol). Phloroglucinol, and its benzenetriol isomers, are still defined as "phenols" according to the IUPAC official nomenclature rules of chemical compounds. Many such monophenolics are often termed polyphenols. The enzyme is biosynthesized by phloroglucinol synthase. Synthesis and occurrence In 1855, phloroglucinol was first prepared from phloretin by the Austrian chemist Heinrich Hlasiwetz (1825–1875). A modern synthesis of phloroglucinol involves hydrolysis of benzene-1,3,5-triamine and its derivatives. Representative is the following route from trinitrobenzene. : The synthesis is noteworthy because ordinary aniline derivatives are unreactive toward hydroxide. Because the tria ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aromatic Ketones
In organic chemistry, aromaticity is a chemical property describing the way in which a conjugated system, conjugated ring of unsaturated bonds, lone pairs, or empty orbitals exhibits a stabilization stronger than would be expected from conjugation alone. The earliest use of the term was in an article by August Wilhelm Hofmann in 1855. There is no general relationship between aromaticity as a chemical property and the olfaction, olfactory properties of such compounds. Aromaticity can also be considered a manifestation of cyclic delocalization and of Resonance (chemistry), resonance. This is usually considered to be because electrons are free to cycle around circular arrangements of atoms that are alternately single- and double-covalent bond, bonded to one another. This commonly seen model of aromatic rings, namely the idea that benzene was formed from a six-membered carbon ring with alternating single and double bonds (cyclohexatriene), was developed by Friedrich August Kekulé ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Antagonists
Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, memory, and physiological processes such as vomiting and vasoconstriction. In the CNS, serotonin regulates mood, appetite, and sleep. Most of the body's serotonin—about 90%—is synthesized in the gastrointestinal tract by enterochromaffin cells, where it regulates intestinal movements. It is also produced in smaller amounts in the brainstem's raphe nuclei, the skin's Merkel cells, pulmonary neuroendocrine cells, and taste receptor cells of the tongue. Once secreted, serotonin is taken up by platelets in the blood, which release it during clotting to promote vasoconstriction and platelet aggregation. Around 8% of the body's serotonin is stored in platelets, and 1–2% is found in the CNS. Serotonin acts as both a vasoconstrictor and vas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
