Abstract：
:The highly rigid and conformationally extended 2-amino-4-phosphonobutanoic acid (AP4) analogue (RS)-1-amino-3-(phosphonomethylene)-cyclobutane-1-carboxylic acid (cyclobutylene AP5) was synthesized and found to inhibit evoked responses in the rat lateral perforant path (LPP) with an IC50 of 41 (+/- 1.5 S.E.M.) microM and the medial perforant pathway with an IC50 of 218 (+/- 3.7 S.E.M.) microM. Furthermore, paired pulse potentiation experiments suggest that cyclobutylene AP5 acts, in part, at a presynaptic site in the LPP. Thus, cyclobutylene AP5 appears to act in a similar manner to L-AP4 in the perforant pathway. These data support the hypothesis that L-AP4 assumes an extended conformation at the L-AP4 receptor of the LPP.
journal_name
Brain Resjournal_title
Brain researchauthors
Peterson NL,Kroona HB,Johnson RL,Koerner JFdoi
10.1016/0006-8993(92)90525-esubject
Has Abstractpub_date
1992-01-31 00:00:00pages
162-4issue
1eissn
0006-8993issn
1872-6240pii
0006-8993(92)90525-Ejournal_volume
571pub_type
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