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.
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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related GABA Receptor Products |
---|
CGP7930
CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. |
5-Aminovaleric acid
5-Aminovaleric acid is a GABA receptor antagonist. |
L-2,4-Diaminobutyric acid dihydrochloride
L-2,4-Diaminobutyric acid dihydrochloride inhibits GABA transaminase activity, resulting in elevated GABA levels, and exhibits ex vivo antitumor activity against mouse fibrosarcoma cells. In addition, L-2,4-Diaminobutyric acid dihydrochloride can be used as an internal standard for amino acid analysis. |
3,4,5-Trimethoxy-trans-cinnamic acid
(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. |
NCS-382 sodium
NCS-382 (sodium) is a potent GABA receptor antagonist. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.