OR-486
OR-486 structure
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Common Name | OR-486 | ||
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| CAS Number | 7659-29-2 | Molecular Weight | 200.10600 | |
| Density | 1.819g/cm3 | Boiling Point | 354.5ºC at 760 mmHg | |
| Molecular Formula | C6H4N2O6 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 162.2ºC | |
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UWA-121, a mixed dopamine and serotonin re-uptake inhibitor, enhances L-DOPA anti-parkinsonian action without worsening dyskinesia or psychosis-like behaviours in the MPTP-lesioned common marmoset.
Neuropharmacology 82 , 76-87, (2014) L-3,4-Dihydroxyphenylalanine (L-DOPA) is the most effective treatment for Parkinson's disease (PD), but its long-term administration is complicated by wearing-off and dyskinesia. UWA-101, a dual, equipotent inhibitor of dopamine (DAT) and serotonin (SERT) tra... |
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Oxidative deamination of noradrenaline in human blood vessels.
J. Neural Transm. Suppl. 32 , 395-404, (1990) Human vascular tissue (saphenous vein and uterine artery) was incubated with tritiated noradrenaline. In both vessels, oxidative deamination predominated over O-methylation. Deamination was due to the action of MAO type A and B, as well as of a semicarbazide-... |
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(−)-Epicatechin in the prevention of tumor necrosis alpha-induced loss of Caco-2 cell barrier integrity
Arch. Biochem. Biophys. 573 , 84-91, (2015) [Display omitted] |
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Catechol-O-methyltransferase (COMT) inhibition reduces spinal nociceptive activity.
Neurosci. Lett. 473(3) , 212-5, (2010) Several variants of the catechol-O-methyltransferase (COMT) gene have recently been linked to pain sensitivity. In the present study, electrophysiological field potential recordings from the dorsal horn in rats were used to examine the spinal effect of reduce... |
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Ultraviolet resonance Raman study of drug binding in dihydrofolate reductase, gyrase, and catechol O-methyltransferase.
Biophys. J. 75(2) , 1097-106, (1998) This paper presents a study of the use of ultraviolet resonance Raman (UVRR) spectroscopic methods as a means of elucidating aspects of drug-protein interactions. Some of the RR vibrational bands of the aromatic amino acids tyrosine and tryptophan are sensiti... |
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Regulation of heme oxygenase-1 expression by dopamine in cultured C6 glioma and primary astrocytes.
Brain Res. Mol. Brain Res. 73(1-2) , 50-9, (1999) Heme oxygenase-1 (HO-1) is an inducible enzyme involved in heme catabolism, tissue iron homeostasis and the cellular response to oxidative stress. Elevated HO-1 expression in astrocytes has been observed in association with abnormal iron deposition and increa... |
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Plasma clearances and extractions of four catecholamines in the anesthetized rabbit: the role of amine removal by blood cells.
J. Cardiovasc. Pharmacol. 21(1) , 21-8, (1993) The purpose of the present study was to compare the plasma kinetics of norepinephrine (NA), epinephrine (A), isoprenaline (ISO), and dopamine (DA) in the anesthetized rabbit. To this end, a mixture of trace amounts of 3H-labeled NA, A, ISO, and DA was infused... |
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Extraneuronal uptake and O-methylation of 3H-adrenaline in the rabbit aorta.
Naunyn Schmiedebergs Arch. Pharmacol. 347(4) , 363-70, (1993) The influence of uptake2 inhibitors on the O-methylation and accumulation of 3H-adrenaline by the isolated rabbit aorta was studied. Strips were incubated with 0.05 mumol/l 3H-(-)-adrenaline during 15 min. Monoamine oxidase and uptake1 were inhibited and the ... |
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COMT-dependent protection of dopaminergic neurons by methionine, dimethionine and S-adenosylmethionine (SAM) against L-dopa toxicity in vitro.
Brain Res. 893(1-2) , 278-81, (2001) L-dopa may be toxic to dopamine neurons, possibly due to catechol-autoxidation. Catechols are O-methylated by catechol-O-methyltransferase (COMT) in a SAM consuming reaction, preventing the initiation of catechol autoxidation. We hypothesized that SAM or SAM-... |
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Properties of novel effective and highly selective inhibitors of catechol-O-methyltransferase.
Life Sci. 43 , 1465, (1988) Novel bisubstituted catechols were found to be potent and highly selective COMT inhibitors in vitro. One of them, OR-462 (3-(3,4-dihydroxy-5-benzylidene)-2,4-pentanedione), was studied also in vivo. When administered to rats orally together with levodopa and ... |