Abstract
The action of two cyclobutane derivatives of l-glutamic acid on the high affinity uptake of l-glutamic acid was investigated using a preparation of synaptosomes from rat cerebral cortex, cis-1-Aminocyclobutane-1,3-dicarboxylic acid (also known as trans-2,4-methanoglutamic acid) potently inhibited l-glutamic acid uptake (IC 50 30 μM), whereas trans-1-aminocyclobutane-1,3-dicarboxylic acid (also known as cis-2,4-methanoglutamic acid), a potent N- methyl- d-aspartate (NMDA) agonist, was inactive. Analysis of the kinetics of l-glutamic acid uptake in the presence and absence of cis-1-aminocyclobutane-1,3-dicarboxylic acid (CACB) suggests that it may act as a competitive inhibitor ( K i 8 μM). CACB may be substrate for the l-glutamic acid high-affinity uptake carrier since preincubation of CACB with the synaptosomal preparation increased its potency in inhibiting l-glutamic acid uptake. The conformationally restricted structure of CACB may be indicative of the conformations of l-glutamic acid that interact with the high affinity uptake carrier.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
