Dihydrokainic acid

Dihydrokainic acid is a glutamate transporters (especially GLT1) inhibitor. Dihydrokainic acid targets GLT1 with high affinity, effectively inhibiting its transport function. Dihydrokainic acid exerts its effect by inhibiting the uptake of glutamate, leading to an increase in extracellular glutamate concentration, thereby affecting neuronal excitability and neurotransmission. Dihydrokainic acid is mainly applied in the field of neuroscience for research on glutamate-related neural functions, epilepsy, learning, and memory^{[1][2][3][4][5]}. IC50 & Target:GLT1^[1] In Vitro:Dihydrokainic acid (5 mM; treating cerebellar slices for 15 min) inhibits the uptake of D-[³H]aspartate by cerebellar slices in a concentration-dependent manner^[2]. In Vivo:Dihydrokainic acid (1-10 mM; perfused through a dialysis probe; for 60 min; single administration) in the rat dentate gyrus model can evoke epileptiform activity, increase the extracellular concentrations of taurine, alanine, phosphoethanolamine, glutamate, and aspartate, increase the amplitude of population spikes and the PS2:PSI ratio^[3]. Dihydrokainic acid (12.5-25 nmol; i.c.v; single administration) in the mouse novel object recognition (NOR) memory model impairs short-term NOR memory performance, long-term NOR memory acquisition, consolidation, and retrieval^[4]. Dihydrokainic acid (1-5 mM; perfused through a dialytrode; for 15 min; single administration) can significantly increase the extracellular concentrations of glutamate and taurine in the rat hippocampus (dentate gyrus or CA1 region) model and reduces the field excitatory postsynaptic potential but increases the population spike, while in the CA1 region, it decreases the amplitudes of both the excitatory postsynaptic potential and the spike in the dentate gyrus^[5].