Name | [(7-nitro-2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methylamino]methylphosphonic acid |
---|---|
Synonyms |
AMP-397A
AMP-397 UNII-X3D0O800AJ {[(7-nitro-2,3-dioxo-1,2,3,4-tetrahydro-quinoxalin-5-ylmethyl)-amino]-methyl}-phosphonic acid N-(2,3-dioxo-7-nitro-1,2,3,4-tetrahydroquinoxalin-5-ylmethyl)aminomethylphosphonic acid N-(7-nitro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-ylmethyl)-aminomethanephosphonic acid Becampanel AMP 397 |
Description | Becampanel (AMP397) is the first competitive AMPA antagonist and an antiepileptic agent. |
---|---|
Related Catalog | |
In Vitro | Becampanel is negative in a mouse lymphoma tk assay, which includes a 24 h treatment without S9. A weak micronucleus induction in vitro is found at the highest concentrations tested in V79 cells with S9[1]. |
In Vivo | Becampanel is negative in the following in vivo studies, which includes the maximum tolerated doses of 320 mg/kg in mice and 2000 mg/kg in rats. Becampanel has no genotoxic potential in vivo[1]. |
Animal Admin | The study protocol is in compliance with the corresponding OECD guideline. The test article is dissolved in 0.2 M NaHCO3. The dose-finding experiment with Becampanel shows that treatment of CD-1 mice by oral gavage with 450.5, 500 or 800 mg/kg, twice with an interval of 24 h, leads to strong signs of toxicity such as laboured breathing, ataxia, and strong sedation. At 320 mg/kg, the same symptoms are visible, but with less severity, and no animals die. On the basis of these results, doses of 32, 100 and 320 mg/kg are chosen for this micronucleus test. In the main experiment five male and five female mice are treated as described above and bone marrow is sampled 48 h after the first application. Nucleated cells are removed from the bone marrow samples using cellulose columns. The cells are loaded on poly-l-lysine coated glass slides by cytocentrifugation using a Shandon Cytospin stained with May Grunwald stain (5%) and Giemsa (14%). The slides are automatically evaluated with a LEITZ MIAS image analyser. No statistical analysis is performed since all values in the treated groups are≤the frequency of micronucleated polychromatic erythrocyte in the concurrent vehicle control group. |
References |
Density | 1.702g/cm3 |
---|---|
Molecular Formula | C10H11N4O7P |
Molecular Weight | 330.19100 |
Exact Mass | 330.03700 |
PSA | 190.91000 |
LogP | 0.26350 |
Index of Refraction | 1.646 |