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Sombrevin

Names

[ CAS No. ]:
1421-14-3

[ Name ]:
Sombrevin

[Synonym ]:
Epontol
Sombrevin
Bayer 1420
Propantan
Fabontal
Fabantol
Propanidid
propanidide

Biological Activity

[Description]:

Propanidid (Sombrevin; Fabantol) is a γ-aminobutyric acid type A (GABAA) receptor agonist and a short-acting non-barbiturate general anesthetic agent. Propanidid can decrease the arterial pressure[1][2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[Target]

GABAA receptor[1]


[In Vivo]

Propanidid (Sombrevin) (3-5 mg/kg; injected into the femoral vein; single dosage) changes the orientation tuning of 58 visual cortex neurons[3]. Animal Model: Adult cats (immobilized by D-tubocurarine)[3] Dosage: 3-5 mg/kg Administration: Injected into the femoral vein; single dosage Result: A reliable change of the preferable orientation by 47.6 ± 5.6 degrees took place in 60% of 58 primary visual cortex neurons, while in the remaining cells it was stable in all stages of anaesthesia. The width of the orientation tuning changed reliably by 65.2 ± 6.7 degrees on the average in 55% of neurons, while in 31% of neurons the tuning acuteness was worse, but in 24% it was sharper. The preferable orientation, the width of the tuning and the frequency of the neuron discharge as a rule recovered in 30 min after the beginning of the anaesthesia.

Chemical & Physical Properties

[ Density]:
1.087g/cm3

[ Boiling Point ]:
459.7ºC at 760mmHg

[ Molecular Formula ]:
C18H27NO5

[ Molecular Weight ]:
337.41100

[ Flash Point ]:
231.8ºC

[ Exact Mass ]:
337.18900

[ PSA ]:
65.07000

[ LogP ]:
2.43810

[ Vapour Pressure ]:
1.24E-08mmHg at 25°C

[ Index of Refraction ]:
1.503

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
AG9625000
CHEMICAL NAME :
Acetic acid, (4-((diethylcarbamoyl)methoxy)-3-methoxyphenyl)-, propyl ester
CAS REGISTRY NUMBER :
1421-14-3
LAST UPDATED :
199612
DATA ITEMS CITED :
8
MOLECULAR FORMULA :
C18-H27-N-O5
MOLECULAR WEIGHT :
337.46
WISWESSER LINE NOTATION :
3OV1R CO1 DO1VN2&2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human
DOSE/DURATION :
5 mg/kg
TOXIC EFFECTS :
Behavioral - general anesthetic Biochemical - Metabolism (Intermediary) - histamines (including liberation not immunochemical in origin)
REFERENCE :
BJANAD British Journal of Anesthesia. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants. RG21 2XS, UK) V.1- 1923- Volume(issue)/page/year: 45,1097,1973
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
81 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AASXAP Acta Anaesthesiologica Scandinavica, Supplementum. (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) No.1- 1959- Volume(issue)/page/year: 17,21,1965
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
113 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,845,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
80 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AASXAP Acta Anaesthesiologica Scandinavica, Supplementum. (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) No.1- 1959- Volume(issue)/page/year: 17,21,1965
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
80 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AASXAP Acta Anaesthesiologica Scandinavica, Supplementum. (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) No.1- 1959- Volume(issue)/page/year: 17,21,1965
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
75 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AASXAP Acta Anaesthesiologica Scandinavica, Supplementum. (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) No.1- 1959- Volume(issue)/page/year: 17,21,1965 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
1200 mg/kg
SEX/DURATION :
female 1-60 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Effects on Newborn - physical
REFERENCE :
NYSJAM New York State Journal of Medicine. (Medical Soc. of the State of New York, POB 5405, Lake Success, NY 11042) V.1- 1901- Volume(issue)/page/year: 64,2177,1964

Safety Information

[ HS Code ]:
2924299090

Synthetic Route

Customs

[ HS Code ]: 2924299090

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%


Related Compounds