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Vigabatrin was found to selectively suppress the late HFOs of ictal complexes. Vigabatrin also suppressed abnormal HFOs recorded during the interictal periods. Thus Vigabatrin was found to be effective in suppressing both the generation of spasms and hypsarrhythmia in the TTX model. Vigabatrin also appears to preferentially suppress the generation of abnormal HFOs, thus implicating neocortical HFOs in the infantile spasms disease state.Although Vigabatrin is associated with retinal dysfunction in patients and Vigabatrin toxicity has been demonstrated by other laboratories in the albino rat, in one pigmented and albino rats, Vigabatrin did not induce deficits in, but rather enhanced, retinal function. Nonetheless, retinal neuronal dysplasia was observed.
 |
Source | Int J Pharm (2014). Figure 2. Vigabatrin |
| Method | LC–MS bioanalysis | |
| Cell Lines | Caco-2 cells | |
| Concentrations | 30 mM | |
| Incubation Time | 6 d | |
| Results | Increasing the concentration of vigabatrin to 30 mM significantly decreased the uptake of Tau to 34 ± 3% |
 |
Source | Int J Pharm (2014). Figure 1. Vigabatrin |
| Method | LC–MS bioanalysis | |
| Cell Lines | Caco-2 cells | |
| Concentrations | 30 mM | |
| Incubation Time | 6 d | |
| Results | Vigabatrin is able to concentration-dependently inhibit the uptake of the prototypic PAT1 substrate proline (Pro) under slightly acidic condition (pH 6.0) in Caco-2 cells yielding an IC50 value of 16.8 mM (logIC50 = 1.2 ± 0.2) with a Hill slope of =0.9±0.3 |
| Cell Experiment | |
|---|---|
| Cell lines | Caco-2 cell |
| Preparation method | The ability of infant formula, Trp, Gly-Gly, Gly-Sar, 2-amino-2-norbornanecarboxylic acid (BCH) and Ile to inhibit the vigabatrin transport in the A–B direction was investigated. NaCl-reduced HBSS containing 1.0 mmol/L vigabatrin and 35.0 mmol/L Trp, 20 mg mL−1 Gly-Gly (151.4 mmol/L), Gly-Sar (136.9 mmol/L), BCH (128.9 mmol/L) or Ile (152.5 mmol/L), with the osmolarity adjusted to 270–310 mOsmol L−1 with mannitol, or H2O containing 1.0 mmol/L vigabatrin and low fat infant formula (150 mg mL−1), with an osmolarity of 310–336 mOsmol L−1 was applied to the apical side of the cells. |
| Concentrations | 1.0 mmol/L |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Sprague-Dawley rats |
| Formulation | |
| Dosages | 200 mg/kg/d |
| Administration | oral |
| Molecular Weight | 129.16 |
| Formula | C6H11NO2 |
| CAS Number | 60643-86-9 |
| Solubility (25°C) | Water 19 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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