Nontransportable blockers of the glutamate transporters are im-portant tools for investigating mechanisms of synaptic transmis-sion. DL-threo--Benzyloxyaspartate (DL-TBOA) is a potent blocker of all subtypes of the excitatory amino acid transporters (EAATs). We characterized novel L-TBOA analogs possessing a substituent on their respective benzene rings. The analogs significantly inhib-ited labeled glutamate uptake, the most potent of which was (2S,3S)-3-{3-[4-(trifluoromethyl)benzoylamino]benzyloxy}aspartate (TFB-TBOA). In an uptake assay using cells transiently expressing EAATs, the IC50 values of TFB-TBOA for EAAT1, EAAT2, and EAAT3 were 22, 17, and 300 nM, respectively. TFB-TBOA was significantly more potent at inhibiting EAAT1 and EAAT...
This work describes the synthesis and initial characterization of the biological activity of a famil...
We characterized the interaction of two conformationally constrained aspartate and glutamate analogs...
Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitor...
Glutamate is the major excitatory neurotransmitter in the mammalian brain. Its rapid clearance after...
Aspartate (Asp) derivatives are privileged compounds for investigating the roles governed by excitat...
The complex amino acid (l-threo)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (l-TFB-TB...
The complex amino acid (L-threo)-3-[3-[4-(trifluoromethyl) benzoylamino] benzyloxy] aspartate (L-TFB...
Excessive glutamate release (mediated by reversed uptake) or impaired reuptake contributes to the et...
Aspartate (Asp) derivatives are privileged compounds for investigating the roles governed by excitat...
In this study we characterized the pharmacological selectivity and physiological actions of a new ar...
Glutamate transporters play an important role in the regulation of extracellular glutamate concentra...
In this study we characterized the pharmacological selectivity and physiological actions of a new ar...
(±)-3-Hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo [3,4 -d]-isoxazole-4-carboxylic acid (HIP-A) and (±)-3...
L-Glutamate is the major excitatory neurotransmitter in the mammalian CNS that can mechanistically c...
Glutamate transporters play important roles in the termination of excitatory neurotransmission and i...
This work describes the synthesis and initial characterization of the biological activity of a famil...
We characterized the interaction of two conformationally constrained aspartate and glutamate analogs...
Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitor...
Glutamate is the major excitatory neurotransmitter in the mammalian brain. Its rapid clearance after...
Aspartate (Asp) derivatives are privileged compounds for investigating the roles governed by excitat...
The complex amino acid (l-threo)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (l-TFB-TB...
The complex amino acid (L-threo)-3-[3-[4-(trifluoromethyl) benzoylamino] benzyloxy] aspartate (L-TFB...
Excessive glutamate release (mediated by reversed uptake) or impaired reuptake contributes to the et...
Aspartate (Asp) derivatives are privileged compounds for investigating the roles governed by excitat...
In this study we characterized the pharmacological selectivity and physiological actions of a new ar...
Glutamate transporters play an important role in the regulation of extracellular glutamate concentra...
In this study we characterized the pharmacological selectivity and physiological actions of a new ar...
(±)-3-Hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo [3,4 -d]-isoxazole-4-carboxylic acid (HIP-A) and (±)-3...
L-Glutamate is the major excitatory neurotransmitter in the mammalian CNS that can mechanistically c...
Glutamate transporters play important roles in the termination of excitatory neurotransmission and i...
This work describes the synthesis and initial characterization of the biological activity of a famil...
We characterized the interaction of two conformationally constrained aspartate and glutamate analogs...
Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitor...