Introduction:Basic information about CAS 58473-74-8|Cinromide, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Cinromide is a broad-spectrum anticonvulsant agent.
Related Catalog
Signaling Pathways >>Others >>OthersResearch Areas >>Neurological Disease
In Vitro
Cinromide (10-100 μM) inhibits 5-HT-induced contractions in rat fundus strips by 46%. Cinromide (100 μM) inhibits monoamine oxidase prepared from both liver and brain of rats[1].
In Vivo
Cinromide shows electroshock convulsion and leptazol(pentetrazo1)-induced convulsion in mice, with ED50s of 60 ± 11 mg/kg, 90 ± 15 mg/kg and 80 ± 15 mg/kg, 300 ± 61 mg/kg for i.p. and oral administrion, respectively. Cinromide produces a dose-related antileptazol activity with an ED50 value of 58 ± 11 mg/kg by i.p. administration in rats. Furthermore, Cinromide (75 mg/kg) significantly elevates the amount of leptazol needed to induce clonic seizures in the intravenously infused leptazol-threshold test in rats. Cinromide (300 mg/kg, i.p) shows no sifnificant effect on the anaesthetized open-chested dogs after 4 h treatment, neither in conscious dogs after 5-h oral treatment with 300 and 600 mg/kg of Cinromide[1]. Cinromide (40 mg/kg, i.v.) depresses the response of the neuron to the unconditioned maxillary nerve stimulus, increasing the latency and decreasing the number of spikes, and depresses the response of the neuron to the unconditioned maxillary nerve stimulus, increasing the latency and decreasing the number of spikes. Cinromide (20, 40, 80 mg/kg, i.v.) increases the latency of the unconditioned response and segmental inhibition dose-dependently. Cinromide decreases periventricular inhibition and EEG[2].
Animal Admin
Cinromide is dissolved in propylene glycol to produce a solution containing 50 mg/mL. It is slowly injected into the femoral vein over a 3-min period. Only one neuron in each cat is studied. To evaluate the dose-response relationship, the drug is given in three cumulative doses. The interval between drug injections is 15 min. Blood samples for drug level measurement are taken 10 min after each injection. Plasma levels of cinromide and its metabolites are determined by high-performance liquid chromotography[2].
[2]. Fromm GH, et al. Effect of cinromide on inhibitory and excitatory mechanisms. Epilepsia. 1983 Aug;24(4):394-400.
Chemical & Physical Properties
Density
1.369g/cm3
Boiling Point
417.5ºC at 760mmHg
Melting Point
89-91ºC(lit.)
Molecular Formula
C11H12BrNO
Molecular Weight
254.12300
Flash Point
206.3ºC
Exact Mass
253.01000
PSA
29.10000
LogP
2.98930
Index of Refraction
1.591
InChIKey
LDCXGZCEMNMWIL-VOTSOKGWSA-N
SMILES
CCNC(=O)C=Cc1cccc(Br)c1
Storage condition
2-8℃
Toxicological Information
CHEMICAL IDENTIFICATION
RTECS NUMBER :
UC6314000
CHEMICAL NAME :
2-Propenamide, 3-(3-bromophenyl)-N-ethyl-, (E)-
CAS REGISTRY NUMBER :
58473-74-8
LAST UPDATED :
199612
DATA ITEMS CITED :
3
MOLECULAR FORMULA :
C11-H12-Br-N-O
MOLECULAR WEIGHT :
254.15
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 :
4437 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
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: 33,741,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
2277 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
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: 33,741,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
660 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
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: 33,741,1981
Safety Information
Symbol
GHS07
Signal Word
Warning
Hazard Statements
H315-H319-H335
Precautionary Statements
P261-P305 + P351 + P338
RIDADR
NONH for all modes of transport
RTECS
UC6314000
HS Code
2924299090
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%
Articles17
More Articles
Prediction of steady-state behavior of metabolite from dosing of parent drug.
J. Pharm. Sci. 69(5) , 610-2, (1980)
Variability in the determination of fraction metabolized in a triangular metabolic problem and its resolution with stable isotope methodology.
J. Pharm. Sci. 73(2) , 285-7, (1984)
Simultaneous determination of the anticonvulsants, cinromide (3-bromo-n-ethylcinnamamide), 3-bromocinnamamide, and carbamazepine in plasma by high-performance liquid chromatography.
J. Chromatogr. A. 163(2) , 187-93, (1979)
A high-performance liquid chromatographic method is described for monitoring plasma concentrations of cinromide (3-bromo-N-ethylcinnamamide) and its de-ethylated metabolite. Carbamazepine levels can b...