Opicapone

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Cat Number

API923287507

CAS Number

923287-50-7

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Product Detail Description Scientific Support Customer Q&A

CAS Number

923287-50-7

Storage

Store at -20°C

Synonyms

BIA 9-1067; 2,5-Dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-4,6-dimethylpyridine 1-oxide; 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxido-3-pyridinyl)-1,2,4-oxadiazol-5-yl]-3-nitro-1,2-benzenediol

Molecular Formula

C15H10Cl2N4O6

Molecular Weight

413.17

Smiles

OC1=CC(C2=NC(C(C(C)=C3Cl)=C([N](=O)=C3C)Cl)=NO2)=CC([N+]([O-])=O)=C1O

General Description

Opicapone (2,5-dichloro-3-[5-(3,4-dihydroxy-5-nitrophenyl]-1,2-4-oxadiazol-3-yl)-4,6-dimethylpyridine 1-oxide) is a new, third-generation, nitrocatechol-based COMT inhibitor. It was approved by the European Medicines Agency in June 2016.

Mechanism of Action

Opicapone is a potent, third-generation peripheral catechol-O-methyltransferase (COMT) inhibitor. Opicapone acts through the reversible inhibition of COMT, an enzyme involved in the metabolism of levodopa in the peripheral circulation. Opicapone prevents the breakdown of levodopa, increasing its bioavailability and prolonging delivery of dopamine to the brain.

Application

Opicapone is used as an adjunct therapy to levodopa/dopa decarboxylase inhibitors in adults with Parkinson’s disease experiencing end-of-dose motor fluctuations.

Opicapone differs from previous-generation nitrocatechols due to its unique 1,2,4-oxadiazole structure and pyridine N-oxide residue. This chemical design enables powerful COMT inhibition while maintaining a favorable safety profile free of cellular toxicity. Notably, it possesses sub-picomolar affinity for peripheral S-COMT but does not cross the blood-brain barrier to affect central COMT levels.

Fig. 1 LD metabolism and place of action of opicapone. (Annus Á, Vécsei L. 2017)

References

Annus Á, Vécsei L. Spotlight on opicapone as an adjunct to levodopa in Parkinson’s disease: design, development and potential place in therapy. Drug Design, Development and Therapy. 2017: 143-151.

Does Opicapone require protection from atmospheric moisture?

Yes, Opicapone is sensitive to humidity and must be kept in airtight containers.

Can Opicapone be stored near volatile organic compounds?

No, Opicapone must be kept away from reactive chemicals to prevent cross-contamination.

Is Opicapone affected by exposure to ultraviolet light?

Yes, Opicapone should be stored in amber-colored or opaque packaging to prevent degradation.

How do I track my Opicapone shipment in real-time?

We provide a digital tracking link for all Opicapone air-freight deliveries.