Study of the stereoselectivity of L-glutamate receptors by synthetic 4(R)- and 4(S)-substituted L-glutamate analogues.
R- and S-stereoisomers of 4-substituted L-glutamate analogues are used to study the stereoselectivity of L-glutamate receptors. It is found that 4(R)-substituted analogues are more potent than their 4(S)-isomers in interacting with L-glutamate receptors both at porcine brain synaptic junctions and on drosophila muscles. This demonstrates that the ligand recognition site of L-glutamate receptors has chiral selectivity discriminating L-glutamate analogues with bulky 4(R)- and 4(S)-substituent groups.
Chang
Y C
YC
Institute of Life Science, National Tsing Hua University, Hsinchu, Taiwan.
Hon
Y S
YS
Chow
W Y
WY
Lin
T A
TA
Cheng
P Y
PY
Wang
C M
CM
D000818:Animals; D001667:Binding, Competitive; D001681:Biological Assay; D004330:Drosophila; D005971:Glutamates / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D007700:Kinetics; D010243:Paralysis; D017470:Receptors, Glutamate / Q000378:metabolism*; D013237:Stereoisomerism; D013552:Swine; D013569:Synapses / Q000378:metabolism
D005971:Glutamates; D017470:Receptors, Glutamate