POLYAMINE AND IFENPRODIL INTERACTIONS WITH THE NMDA RECEPTORS GLYCINE SITE

被引:29
作者
RANSOM, RW
机构
[1] Merck Sharp and Dohme Research Laboratories, Department of New Lead Pharmacology, West Point
来源
EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION | 1991年 / 208卷 / 01期
关键词
N-METHYL-D-ASPARTATE (NMDA); IFENPRODIL; POLYAMINES; GLYCINE;
D O I
10.1016/0922-4106(91)90052-J
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Ifenprodil partially inhibited [H-3]glycine binding to the N-methyl-D-aspartate (NMDA) receptor in rat telencephalic membranes. The polyamine spermine significantly enhanced [H-3]glycine binding and decreased ifenprodils inhibitory potency. However, ifenprodil was unable to completely reverse the stimulation of binding produced by spermine. Also, ifenprodil was found to reduce the maximum degree to which spermine enhanced binding but had no effect on the polyamine's potency. These results show that ifenprodil and spermine do not competitively interact with respect to their abilities to modify [H-3]glycine binding to the NMDA receptor complex.
引用
收藏
页码:67 / 71
页数:5
相关论文
共 17 条
[1]   IFENPRODIL AND SL-82.0715 ARE ANTAGONISTS AT THE POLYAMINE SITE OF THE N-METHYL-D-ASPARTATE (NMDA) RECEPTOR [J].
CARTER, C ;
RIVY, JP ;
SCATTON, B .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1989, 164 (03) :611-612
[2]  
CARTER C, 1988, J PHARMACOL EXP THER, V247, P1222
[3]  
CARTER CJ, 1990, J PHARMACOL EXP THER, V253, P475
[4]  
LOWRY OH, 1951, J BIOL CHEM, V193, P265
[5]   [-3H]GLYCINE BINDING IS MODULATED BY MG-2+ AND OTHER LIGANDS OF THE NMDA RECEPTOR-CATION CHANNEL COMPLEX [J].
MARVIZON, JCG ;
SKOLNICK, P .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1988, 151 (01) :157-158
[6]   ANALYSIS OF RADIOLIGAND BINDING EXPERIMENTS - A COLLECTION OF COMPUTER-PROGRAMS FOR THE IBM-PC [J].
MCPHERSON, GA .
JOURNAL OF PHARMACOLOGICAL METHODS, 1985, 14 (03) :213-228
[7]   POLYAMINES REGULATE GLYCINE INTERACTION WITH THE N-METHYL-D-ASPARTATE RECEPTOR [J].
RANSOM, RW ;
DESCHENES, NL .
SYNAPSE, 1990, 5 (04) :294-298
[8]   COOPERATIVE MODULATION OF [H-3] MK-801 BINDING TO THE N-METHYL-D-ASPARTATE RECEPTOR-ION CHANNEL COMPLEX BY L-GLUTAMATE, GLYCINE, AND POLYAMINES [J].
RANSOM, RW ;
STEC, NL .
JOURNAL OF NEUROCHEMISTRY, 1988, 51 (03) :830-836
[9]   ARCAINE IS A COMPETITIVE ANTAGONIST OF THE POLYAMINE SITE ON THE NMDA RECEPTOR [J].
REYNOLDS, IJ .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1990, 177 (03) :215-216
[10]  
REYNOLDS IJ, 1990, J PHARMACOL EXP THER, V255, P1001