ACTIVITY OF THE CONFORMATIONALLY RIGID 2-AMINO-4-PHOSPHONOBUTANOIC ACID (AP4) ANALOG (RS)-1-AMINO-3-(PHOSPHONOMETHYLENE)CYCLOBUTANE-1-CARBOXYLIC ACID (CYCLOBUTYLENE AP5) ON EVOKED-RESPONSES IN THE PERFORANT PATHWAY OF RAT HIPPOCAMPUS

被引:11
作者
PETERSON, NL
KROONA, HB
JOHNSON, RL
KOERNER, JF
机构
[1] UNIV MINNESOTA,DEPT BIOCHEM,4-225 MILLARD HALL,435 DELAWARE ST SE,MINNEAPOLIS,MN 55455
[2] UNIV MINNESOTA,DEPT MED CHEM,MINNEAPOLIS,MN 55455
关键词
L-2-AMINO-4-PHOSPHONOBUTANOIC ACID RECEPTOR; L-2-AMINO-4-PHOSPHONOBUTANOIC ACID; LATERAL PERFORANT PATH; HIPPOCAMPUS;
D O I
10.1016/0006-8993(92)90525-E
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
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.) mu-M and the medial perforant pathway with an IC50 of 218 (+/- 3.7 S.E.M.) mu-M. 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.
引用
收藏
页码:162 / 164
页数:3
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