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.

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Enzymes involved in neurotransmission. From Wikipedia, the free encyclopedia. COMT inhibitors include tolcaponeentacapone and opicaponewhich are used in the treatment of Parkinson’s disease.

Catechol-O-methyltransferase – Wikipedia

Journal of Oral Rehabilitation. December Learn how and when to remove this template message. In other projects Wikimedia Commons.

This page was last edited on 21 Novemberat For tolcapone and mg have most often proved to be the optimal doses. Retrieved November 16, American Journal of Human Genetics.

The enzyme introduces a methyl group to the catecholamine, which is donated by S-adenosyl methionine SAM. They induce a dose-dependent inhibition of COMT activity in erythrocytes and a significant decrease in the plasma levels of 3-O-methyldopa, indicating their effectiveness as COMT inhibitors.

The British Journal of Psychiatry. 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 comtt of catecholamines. Consequently, they increase the elimination half-life of levodopa and thus prolong the availability of levodopa to the brain without significantly affecting the Cmax or tmax of levodopa.


EC number Enzyme superfamily Enzyme family List of enzymes. Chromosome 22 human [1]. The best-studied is ValMet. When given with an inhibitor of dopa decarboxylase carbidopa or benserazidelevodopa is optimally saved.

Aspartate carbamoyltransferase Ornithine carbamoyltransferase Oxamate carbamoyltransferase Putrescine carbamoyltransferase 3-hydroxymethylcephem carbamoyltransferase Lysine carbamoyltransferase N-acetylornithine carbamoyltransferase. However, there seems to be a trend for tolcapone to induce more often diarrhoea and increase in liver transaminases compared with entacapone. The Journal of Biological Chemistry. Thus, COMT inhibitors are clinically significant and beneficial adjunct to levodopa therapy in Parkinson’s disease patients with end-of-dose fluctuations.

Molecular and Cellular Biology lq. 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. Inhiibdores article relies too much on references to primary sources.

Levodopaa precursor of catecholamines, is an important substrate of COMT. Cholinesterase AcetylcholinesteraseButyrylcholinesterase. Lay summary — MedWireNews. Both pharmacokinetically and clinically the mg dose of entacapone is the most effective dose compared with placebo. Phosphoribosylglycinamide formyltransferase Inosine monophosphate synthase. Oroszi G, Goldman D December The gene is associated with allelic variants. Catechol- O -methyltransferase is involved in the inactivation of the catecholamine neurotransmitters dopamineepinephrineand norepinephrine.

The effect size of cpmt moderation was quite large: Entacapone acts mainly peripherally whereas tolcapone acts both peripherally and centrally. However, tolcapone is clinically restricted owning to its increased hepatotoxicity and other related digestive disorders.

The dyskinesias are managed by decreasing the daily levodopa dose in Parkinson’s disease patients with end-of-dose fluctuations. All articles with dead external links Articles with dead external links from November Articles with permanently dead external links Articles lacking reliable references from December All articles lacking reliable references Commons category link is on Wikidata.


Both entacapone and tolcapone are well-tolerated.

Views Read Edit View history. Comparable effects inhibieores similar cognitive tasks, the frontal lobes, and the neurotransmitter dopamine have also all been linked to schizophrenia.

By using this site, you agree to the Terms of Use and Privacy Policy. Genes on human chromosome 22 EC 2. Retrieved from ” https: Please improve this by adding secondary or tertiary sources. It is increasingly recognised that allelic variation at the COMT gene are also relevant for emotional inhibidoree, as they seem to influence the interaction between prefrontal and limbic regions.

Goetz CG May Tyrosine hydroxylase Aromatic L-amino acid decarboxylase Dopamine beta-hydroxylase Phenylethanolamine N-methyltransferase. Their effects and significance also in the treatment of de novo patients need to be clarified.

This “triple therapy” is becoming a standard in the treatment of Parkinson’s disease.

COMT inhibition in the treatment of Parkinson’s disease.

Any compound having a catechol structure, like catecholestrogens and catechol-containing flavonoids, are substrates of COMT. 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. Zhu BT October Available structures PDB Ortholog search: The Central Nervous System. Histamine N-methyltransferase Phenylethanolamine N-methyltransferase Amine N-methyltransferase Phosphatidylethanolamine N-methyltransferase.