Nitecapone

Modify Date: 2024-01-11 15:29:06

Nitecapone Structure
Nitecapone structure
Common Name Nitecapone
CAS Number 116313-94-1 Molecular Weight 265.21900
Density 1.451g/cm3 Boiling Point 495.3ºC at 760 mmHg
Molecular Formula C12H11NO6 Melting Point N/A
MSDS Chinese USA Flash Point 211.6ºC
Symbol GHS06
GHS06
Signal Word Danger

 Use of Nitecapone


Nitecapone (OR-462) is an orally active and short-acting catechol-O-methyltransferase (COMT) inhibitor with gastroprotective and antioxidant properties. Nitecapone (OR-462) scavenges reactive oxygen and nitric radicals and prevents lipid peroxidation[1][2][3].

 Names

Name 3-[(3,4-dihydroxy-5-nitrophenyl)methylidene]pentane-2,4-dione
Synonym More Synonyms

 Nitecapone Biological Activity

Description Nitecapone (OR-462) is an orally active and short-acting catechol-O-methyltransferase (COMT) inhibitor with gastroprotective and antioxidant properties. Nitecapone (OR-462) scavenges reactive oxygen and nitric radicals and prevents lipid peroxidation[1][2][3].
Related Catalog
In Vitro Nitecapone (1-100 μM) reducesd GSH (reduced glutathione) depletion induced by ROO-by 11-38% and oxidation to oxidized glutathione (GSSG) by 32-45%[1].
In Vivo Nitecapone (30 mg/kg, ip daily for 13 days) reduces development and symptoms of neuropathic pain after spinal nerve ligation in rats[3]. Animal Model: Eighty-six male Wistar rats, weighing 140-350 g[3]. Dosage: 30 mg/kg (3.3 mL/kg). Administration: IP, once daily for 13 days. Result: Selectively and specifically inhibits COMT in the peripheral tissues, and to some extent in the CNS for ca. 3 h. Increased the thresholds for the mechanical stimuli and thus reduced mechanical allodynia. Reduced the number of positive reactions of the ipsilateral paws when compared with the baselines in the nitecapone-pretreated rats.
References

[1]. Y J Suzuki, et al. Antioxidant properties of nitecapone (OR-462). Free Radic Biol Med. 1992 Nov;13(5):517-25.

[2]. Marcocci L, et al. Nitecapone: a nitric oxide radical scavenger. Biochemistry and Molecular Biology International, 01 Oct 1994, 34(3):531-541.

[3]. Oleg Kambur, et al. Nitecapone reduces development and symptoms of neuropathic pain after spinal nerve ligation in rats. Eur J Pain. 2011 Aug;15(7):732-40.

 Chemical & Physical Properties

Density 1.451g/cm3
Boiling Point 495.3ºC at 760 mmHg
Molecular Formula C12H11NO6
Molecular Weight 265.21900
Flash Point 211.6ºC
Exact Mass 265.05900
PSA 120.42000
LogP 2.09060
Vapour Pressure 1.95E-10mmHg at 25°C
Index of Refraction 1.645

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SA1942500
CHEMICAL NAME :
2,4-Pentanedione, 3-((3,4-dihydroxy-5-nitrophenyl)methylene)-
CAS REGISTRY NUMBER :
116313-94-1
LAST UPDATED :
199612
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C12-H11-N-O6
MOLECULAR WEIGHT :
265.24

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PHTOEH Pharmacology and Toxicology (Copenhagen). (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.60- 1987- Volume(issue)/page/year: 69,64,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
507 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PHTOEH Pharmacology and Toxicology (Copenhagen). (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.60- 1987- Volume(issue)/page/year: 69,64,1991

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
RIDADR UN 2811 6.1 / PGIII

 Articles22

More Articles
D1-like dopamine receptor activation and natriuresis by nitrocatechol COMT inhibitors.

Kidney Int. 59(5) , 1683-94, (2001)

In recent years, several nitrocatechol derivatives (tolcapone, entacapone, and nitecapone) have been developed and found to be highly selective and potent inhibitors of catechol-O-methyltransferase (C...

Extending levodopa action: COMT inhibition.

Neurology 50(6 Suppl 6) , S27-32; discussion S44-8, (1998)

Degradation of levodopa in the periphery is known to be associated with motor fluctuations and dyskinesia in Parkinson's disease (PD) patients. The enzyme catechol-O-methyltransferase (COMT) is respon...

The Helicobacter felis mouse model in assessing anti-Helicobacter therapies and gastric mucosal prostaglandin E2 levels.

Scand. J. Gastroenterol. 31(4) , 334-8, (1996)

The aims of the present study were to assess the usefulness of the Helicobacter felis mouse model in the evaluation of antimicrobial therapies and the effect of Helicobacter infection on gastric mucos...

 Synonyms

3-(3,4-dihydroxy-5-nitrobenzylidene)-2,4-pentanedione
2,4-Pentanedione,3-((3,4-dihydroxy-5-nitrophenyl)methylene)
Nitecapone
3-(3,4-dihydroxy-5-nitrophenyl)methylene-2,4-pentanedione
Nitecapona [INN-Spanish]
Nitecapone [INN]
OR 462
Nitecaponum [INN-Latin]
Top Suppliers:I want be here




Get all suppliers and price by the below link:

Nitecapone suppliers


Price: ¥2100/5 mg

Reference only. check more Nitecapone price