Back to Search
Start Over
A rational approach to the design of selective substrates and potent nontransportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3). new glutamate and aspartate analogues as potential neuroprotective agents
- Publication Year :
- 2001
-
Abstract
- Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitors have been developed, and new glutamate (Glu) and aspartate (Asp) analogues have been synthesized. The analogues 1a and 3 represent novel lead compounds for the development of EAAT substrates and nontransportable inhibitors, selective for EAATs over iGluRs, as possible neuroprotective agents useful to minimize the progression of chronic or acute neurodegenerative diseases. The role played by the protonatable amine function in the interaction with EAATs has been discussed.
- Subjects :
- Models, Molecular
Patch-Clamp Techniques
Molecular model
Amino Acid Transport System X-AG
Molecular Conformation
In Vitro Techniques
Chemical synthesis
Neuroprotection
Glutamate Plasma Membrane Transport Proteins
Radioligand Assay
Structure-Activity Relationship
chemistry.chemical_compound
Glutamates
Drug Discovery
Animals
Neurotransmitter
Cerebral Cortex
Aspartic Acid
Symporters
biology
Chemistry
Excitatory amino-acid transporter
Sodium
Glutamate receptor
Biological Transport
In vitro
Rats
Excitatory Amino Acid Transporter 3
Neuroprotective Agents
Biochemistry
Drug Design
biology.protein
Molecular Medicine
Carrier Proteins
Function (biology)
Subjects
Details
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....fac912a58677d7f34f87209a4713851e