glutamate uptake

Cis-ACBD (cis-1-aminocyclobutane-1,3-dicarboxylic acid) is a potent and selective N-methyl-D-aspartate receptor agonist.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Afoxolaner is an isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

BCATc Inhibitor 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. BCATc Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective e

EAAT2(GLT1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake

inhibitor of both glial and neuronal uptake of glutamate, aspartate and cysteate.

WAY-855 is an EAAT2-preferring, nonsubstrate inhibitor of high-affinity glutamate uptake.

DL-TBOA ammonium is a potent, non-transportable inhibitor of excitatory amino acid transporters. Its inhibitory effects are demonstrated by IC50 values of 70 μM, 6 μM, and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2, and EAAT3, respectively. Additionally, DL-TBOA ammonium significantly hampers the uptake of [14C]glutamate in COS-1 cell lines expressing human EAAT1 and EAAT2, evident by Ki values of 42 μM and 5.7 μM, respectively. Furthermore, this compound competitively blocks EAAT4 and EAAT5, with Ki values of 4.4 μM and 3.2 μM, respectively.

Nε-(1-Carboxyethyl)-L-lysine (CEL) is an advanced glycation end-product (AGE), resulting from the chemical modification of proteins by methylglyoxal. Exposure to CEL reduces glutamate uptake and S100B secretion in the hippocampus, making it useful for studying ageing, metabolism, and diabetes.

Zonisamide-d4 is a deuterated compound of Zonisamide. Zonisamide has a CAS number of 68291-97-4. Zonisamide, a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Troriluzole hydrochloride is the third-generation tripeptide precursor of Riluzole and acts as an orally active glutamate modulator. It reduces synaptic glutamate levels while enhancing glutamate uptake. Troriluzole hydrochloride has potential applications for treating Alzheimer's disease and generalized anxiety disorder (GAD).