Síntesis de nitroderivados de hidroxitirosol como potenciales inhibidores de COMT. Article in Basic & Clinical Pharmacology & Toxicology · January . The principle aim of COMT inhibitor therapy is to increase the duration of El principal objetivo del tratamiento con inhibidores de la COMT es. AMPT: α-metil-p-tirosina; COMT: catecol-O- . gena en la circulación, primero son metiladas por la COMT y con- Existen también inhibidores de la 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. Catechol- O -methyltransferase is involved in the inactivation of the catecholamine neurotransmitters dopamineepinephrineand norepinephrine. The enzyme introduces a methyl group to the catecholamine, which is donated by S-adenosyl methionine SAM. Any compound having a catechol structure, like catecholestrogens and catechol-containing flavonoids, are substrates of COMT.
Levodopaa precursor of catecholamines, is an important substrate of COMT.
When given with an inhibitor of dopa decarboxylase carbidopa or benserazidelevodopa is optimally saved. This “triple therapy” is becoming a standard in the treatment of Parkinson’s disease. In the brain, COMT-dependent dopamine degradation is of particular importance in brain regions with low expression of the presynaptic dopamine transporter DATsuch as the prefrontal cortex.
The gene is associated with allelic variants. The best-studied is ValMet. A functional single-nucleotide polymorphism a common normal variant of the gene for catechol-O-methyltransferase results in a valine to methionine mutation at position Val Met rs Given the preferential role of COMT in prefrontal dopamine degradation, the ValMet polymorphism is thought to exert its effects on cognition by modulating dopamine signaling in the frontal lobes. The gene variant has been shown to affect cognitive tasks broadly related to executive functionsuch as set shifting, response inhibition, abstract thought, and the acquisition of rules or task structure.
ES2282924T3 – Inhibidores de la comt. – Google Patents
Comparable effects on similar cognitive tasks, the frontal lobes, and the neurotransmitter dopamine have also all been linked to schizophrenia. It is increasingly inhibidkres that inhibidoores variation at the COMT gene are also relevant for emotional processing, as they seem to influence the interaction between prefrontal and limbic regions. Research conducted at the Section of Neurobiology of Psychosis inhibisores, Institute of Psychiatry, King’s College London has demonstrated an effect of COMT both in patients with bipolar disorder and in their relatives,  [ unreliable medical source ] but these findings have not been replicated so far.
The effect size of genotypic moderation was quite large: Genetic variation with functional impact on cortical dopamine tone has a strong influence on reward experience in the flow of daily life. Temporomandibular joint dysfunction TMD does not appear to be a classic genetic disorder, however variations in the gene that codes for COMT have been suggested to be responsible for inheritance of a predisposition to develop TMD during life.
COMT is the name given to the gene that codes for this inhibidorres. The O in the name stands for oxygennot for ortho. COMT inhibitors include tolcaponeentacapone and opicaponewhich are used in the treatment of Parkinson’s disease.
COMT inhibition in the treatment of Parkinson’s disease.
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Catechol-O-methyltransferase – Wikipedia
Student consult 7th ed. Retrieved November 16, Goetz CG May Neurotransmitters and their receptors”. The Central Nervous System. The Journal of Biological Chemistry. Principles of pharmacology 3rd ed. Journal of Alzheimer’s Disease. The American Journal of Psychiatry. American Journal of Human Genetics. The British Journal of Psychiatry. Lay summary — MedWireNews. Journal dw Oral Rehabilitation. Two of the nitrocatechols, entacapone However, tolcapone is clinically restricted owning to its vomt hepatotoxicity and other related digestive disorders.
EC number Enzyme superfamily Enzyme family List of enzymes. Molecular and Cellular Biology portal. Retrieved from ” https: Genes on human chromosome 22 EC 2.
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