Vigabatrin is an irreversible inhibitor of γ-aminobutyric acid transaminase (GABA-T), with potent activity in elevating brain GABA levels and enhancing inhibitory neurotransmission [1-3]. Vigabatrin is commonly used to treat refractory epilepsy [4].
In glioblastoma multiforme cell (13–06-MG), concentration-dependent inhibitory effect of Vigabatrin (0.3-100μM; 24h) on the activity of IKCa channels [5]. In Caco-2 and MDCK cells, Vigabatrin (30mM; 24h) inhibits the uptake of taurine in Caco-2 and MDCK cells to 34 ± 3 and 53 ± 2% [6]. In U87 cells, Vigabatrin administration has a growth-promoting effect on cells [7].
In Tsc1GFAPCKO mice, Vigabatrin (50mg/kg, 100mg/kg, 200mg/kg; ip; 10 weeks) treatment decreased the development of seizures and modestly improved survival [8]. In C57BL/6J mice, after of Vigabatrin (140mg/kg; ip; 4 weeks) treatment, ERG b-wave amplitude was enhanced, and amplitudes of oscillatory potentials were reduced [9]. In C57BL/6J mice, Vigabatrin (35-140mg/kg; sc; 14d) treatment induces amino acid disturbances in mice [10].
References:
[1]. French JA. Vigabatrin. Epilepsia. 1999 May; 40: s11-6.
[2]. James Willmore L, Abelson MB, Ben‐Menachem E, et al. Vigabatrin: 2008 update. Epilepsia. 2009 Feb; 50(2): 163-173.
[3]. Ben‐Menachem E. Mechanism of action of vigabatrin: correcting misperceptions. Acta neurologica scandinavica. 2011 Dec; 124: 5-15.
[4]. Tartara A, Manni R, Galimberti CA, et al. Vigabatrin in the treatment of epilepsy: a double‐blind, placebo‐controlled study. Epilepsia. 1986 Dec; 27(6): 717-723.
[5]. Hung TY, Huang HY, Wu SN, et al. Depressive effectiveness of vigabatrin (γ-vinyl-GABA), an antiepileptic drug, in intermediate-conductance calcium-activated potassium channels in human glioma cells. BMC Pharmacology and Toxicology. 2021 Dec; 22: 1-9.
[6]. Plum J, Nøhr MK, Hansen SH, et al. The anti-epileptic drug substance vigabatrin inhibits taurine transport in intestinal and renal cell culture models. International journal of pharmaceutics. 2014 Oct 1; 473(1-2): 395-397.
[7]. Lee CY, Lai HY, Chiu A, et al. The effects of antiepileptic drugs on the growth of glioblastoma cell lines. Journal of neuro-oncology. 2016 May; 127: 445-453.
[8]. Zhang B, McDaniel SS, Rensing NR, et al. Vigabatrin inhibits seizures and mTOR pathway activation in a mouse model of tuberous sclerosis complex. PLoS One. 2013 Feb 20; 8(2): e57445.
[9]. Chan K, Hoon M, Pattnaik BR, et al. Vigabatrin-induced retinal functional alterations and second-order neuron plasticity in C57BL/6J mice. Investigative Ophthalmology & Visual Science. 2020 Feb 7; 61(2): 17.
[10]. Walters DC, Arning E, Bottiglieri T, et al. Metabolomic analyses of vigabatrin (VGB)-treated mice: GABA-transaminase inhibition significantly alters amino acid profiles in murine neural and non-neural tissues. Neurochemistry international. 2019 May 1; 125: 151-162.
















