OR-486

Catechol O-methyltransferase inhibitor CAS# 7659-29-2

OR-486

Catalog No. BCC5661----Order now to get a substantial discount!

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Quality Control of OR-486

Number of papers citing our products

Chemical structure

OR-486

3D structure

Chemical Properties of OR-486

Cas No. 7659-29-2 SDF Download SDF
PubChem ID 1810907 Appearance Powder
Formula C6H4N2O6 M.Wt 200.11
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in ethanol and to 100 mM in DMSO
Chemical Name 3,5-dinitrobenzene-1,2-diolate
SMILES C1=C(C=C(C(=C1[N+](=O)[O-])[O-])[O-])[N+](=O)[O-]
Standard InChIKey VDCDWNDTNSWDFJ-UHFFFAOYSA-L
Standard InChI InChI=1S/C6H4N2O6/c9-5-2-3(7(11)12)1-4(6(5)10)8(13)14/h1-2,9-10H/p-2
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of OR-486

DescriptionPotent and selective inhibitor of catechol-O-methyl-transferase.

OR-486 Dilution Calculator

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OR-486 Molarity Calculator

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Preparing Stock Solutions of OR-486

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.9973 mL 24.9863 mL 49.9725 mL 99.945 mL 124.9313 mL
5 mM 0.9995 mL 4.9973 mL 9.9945 mL 19.989 mL 24.9863 mL
10 mM 0.4997 mL 2.4986 mL 4.9973 mL 9.9945 mL 12.4931 mL
50 mM 0.0999 mL 0.4997 mL 0.9995 mL 1.9989 mL 2.4986 mL
100 mM 0.05 mL 0.2499 mL 0.4997 mL 0.9995 mL 1.2493 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on OR-486

Hispidulin alleviated methamphetamine-induced hyperlocomotion by acting at alpha6 subunit-containing GABAA receptors in the cerebellum.[Pubmed:27385415]

Psychopharmacology (Berl). 2016 Sep;233(17):3187-99.

RATIONALE: Hispidulin is a flavonoid we isolated from Clerodendrum inerme, an herb that effectively remitted a case of intractable motor tic disorders. Hispidulin was shown to be a positive allosteric modulator (PAM) of GABAA receptors, including the alpha6 subunit-containing subtype (alpha6GABAAR) that is predominantly expressed in cerebellar granule cells and insensitive to diazepam. OBJECTIVES: We explored the action mechanism(s) of hispidulin using hyperdopaminergic mouse models induced by methamphetamine and apomorphine, based on the hyperdopaminergic nature of tic disorders. RESULTS: Hispidulin significantly inhibited methamphetamine-induced hyperlocomotion (MIH) at i.p. doses without affecting apomorphine-induced hyperlocomotion and stereotypy behaviors or having significant benzodiazepine-like effects (BZLE), including sedation, anxiety, and motor impairment. When given by intracerebellar (i.c.b.) microinjection, hispidulin also alleviated MIH and this effect was prevented by i.c.b. coadministration of furosemide, an alpha6GABAAR antagonist, and mimicked by i.c.b. Ro 15-4513, an alpha6GABAAR PAM. Conversely, i.c.b. diazepam did not affect MIH while it reduced MIH at i.p. doses having significant BZLE. In a screening assay for 92 neurotransmitter receptors/degradation enzymes/transporters, hispidulin displayed significant (>50 % inhibition of radiolabeled ligand binding at 10 muM) binding affinity only at the benzodiazepine binding site of GABAARs (IC50 0.73 approximately 1.78 muM) and catecholamine-o-methyl-transferase (COMT) (IC50 1.32 muM). OR-486, a more potent COMT inhibitor than hispidulin, did not affect MIH. CONCLUSIONS: It is suggested that hispidulin alleviates MIH via acting as a PAM of cerebellar alpha6GABAARs, but not through COMT inhibition or affecting dopamine receptor responsiveness. Thus, selective alpha6GABAAR PAMs may have the potential to be a novel treatment for hyperdopaminergic disorders.

Inhibitors of catechol-O-methyltransferase sensitize mice to pain.[Pubmed:20726980]

Br J Pharmacol. 2010 Dec;161(7):1553-65.

BACKGROUND AND PURPOSE: Catechol-O-methyltransferase (COMT) inhibitors are used in Parkinson's disease in which pain is an important symptom. COMT polymorphisms modulate pain and opioid analgesia in humans. In rats, COMT inhibitors have been shown to be pro-nociceptive in acute pain models, but also to attenuate allodynia and hyperalgesia in a model of diabetic neuropathy. Here, we have assessed the effects of acute and repeated administrations of COMT inhibitors on mechanical, thermal and carrageenan-induced nociception in male mice. EXPERIMENTAL APPROACH: We used single and repeated administration of a peripherally restricted, short-acting (nitecapone) and also a centrally acting (3,5-dinitrocatechol, OR-486) COMT inhibitor. We also tested CGP 28014, an indirect inhibitor of COMT enzyme. Effects of OR-486 on thermal nociception were also studied in COMT deficient mice. Effects on spinal pathways were assessed in rats given intrathecal nitecapone. KEY RESULTS: After single administration, both nitecapone and OR-486 reduced mechanical nociceptive thresholds and thermal nociceptive latencies (hot plate test) at 2 and 3 h, regardless of their brain penetration. These effects were still present after chronic treatment with COMT inhibitors for 5 days. Intraplantar injection of carrageenan reduced nociceptive latencies and both COMT inhibitors potentiated this reduction without modifying inflammation. CGP 28014 shortened paw flick latencies. OR-486 did not modify hot plate times in Comt gene deficient mice. Intrathecal nitecapone modified neither thermal nor mechanical nociception. CONCLUSIONS AND IMPLICATIONS: Pro-nociceptive effects of COMT inhibitors were confirmed. The pro-nociceptive effects were primarily mediated via mechanisms acting outside the brain and spinal cord. COMT protein was required for these actions.

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