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2H-1,3-Oxazine-2,4(3H)-dione,5,5-diethyldihydro-

Names

[ CAS No. ]:
702-54-5

[ Name ]:
2H-1,3-Oxazine-2,4(3H)-dione,5,5-diethyldihydro-

[Synonym ]:
Dietadione [Italian]
Diethadione
Dioxone
Persisten
5,5-diethyldihydro-2H-1,3-oxazine-2,4(3H)-dione
5,5-Diaethyl-dihydro-[1,3]oxazin-2,4-dion
Toce
5,5-diethyl-[1,3]oxazinane-2,4-dione
DIETHADION
Tocen
Lepton
Ledosten
Dietroxin
5,5-diethyl-dihydro-[1,3]oxazine-2,4-dione

Biological Activity

[Description]:

Dioxone is a substance possessing convulsant properties qualitatively similar to leptazol and bemegride. Dioxone is orally active[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[In Vitro]

Dioxone is soluble in ethanol, ether, chloroform and propylene glycol. A 1 percent aqueous solution may be obtained at room temperature giving a pH of 4.3, and, with warming to 50℃, 2 percent aqueous solutions may be prepared[1].

[In Vivo]

Dioxone (0-30 mg/kg; i.v., i.p., oral, s.c.; once) induces convulsant action[1]. Animal Model: CF-1 Mice and CF-Wistar rats[1] Dosage: 0-30 mg/kg Administration: Intraperitoneal injection, once Result: In mice: The spontaneous activity was often reduced, always accompanied by hyperreactivity at 10 mg/kg, tremors, clonic convulsion and motor incoordination phenomena occured after the administration of 30 mg/kg. In rats: Tremors and some isolated clonus of the muscles of the limbs were observed with 10 mg/kg, clonic convukions occurred with doses above 15 mg/kg.

[References]

[1]. G MAFFII, et al. A new analeptic: 5, 5-diethyl-1, 3-oxazine-2,4-dione (Dioxone). J Pharm Pharmacol. 1961 Apr;13:244-53.

Chemical & Physical Properties

[ Density]:
1.069g/cm3

[ Molecular Formula ]:
C8H13NO3

[ Molecular Weight ]:
171.19

[ Exact Mass ]:
171.09000

[ PSA ]:
55.40000

[ LogP ]:
1.38800

[ Index of Refraction ]:
1.44

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
RP6300000
CHEMICAL NAME :
2H-1,3-Oxazine-2,4(3H)-dione, 5,5-diethyldihydro-
CAS REGISTRY NUMBER :
702-54-5
BEILSTEIN REFERENCE NO. :
0133129
LAST UPDATED :
199701
DATA ITEMS CITED :
10
MOLECULAR FORMULA :
C8-H13-N-O3
MOLECULAR WEIGHT :
171.22
WISWESSER LINE NOTATION :
T6OVMVTJ E2 E2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
71 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 13,244,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
32 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 13,244,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
39 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 13,244,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
81 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,282,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
49 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,281,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
61 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,281,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
32 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 13,244,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
45 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,282,1970 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
4550 mg/kg/26W-I
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Related to Chronic Data - death
REFERENCE :
JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 13,244,1961

Related Compounds