COOPERATIVE INTERACTIONS AT [KAINIC-H-3 ACID BINDING-SITES IN RAT AND HUMAN CEREBELLUM

被引:43
作者
LONDON, ED
COYLE, JT
机构
[1] JOHNS HOPKINS UNIV,SCH MED,DEPT PHARMACOL,BALTIMORE,MD 21205
[2] JOHNS HOPKINS UNIV,SCH MED,DEPT EXPTL THERAPEUT,BALTIMORE,MD 21205
[3] JOHNS HOPKINS UNIV,SCH MED,DEPT PSYCHIAT,BALTIMORE,MD 21205
[4] JOHNS HOPKINS UNIV,SCH MED,DEPT BEHAV SCI,BALTIMORE,MD 21205
关键词
Cerebellum; Cooperativity; Dihydrokainic acid; Glutamic acid; Kainic acid; Receptor binding;
D O I
10.1016/0014-2999(79)90186-9
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Inhibition of the specific binding of [3H]kainic acid was studied in membranes isolated from rat and human cerebellum; the sequence of potencies in both species were: kainic acid > L-glutamic acid > dihydrokainic acid > D-glutamic acid. Whereas the Hill coefficient for unlabelled Kainate was 1.0, dihydrokainic acid and D- and L-glutamic acids exhibited negative cooperativity with Hill coefficients of near 0.5. This allosteric interaction of glutamic acid at the kainic acid recognition site suggests a biochemical correlate for the synergistic effects of these compounds in vivo. © 1979.
引用
收藏
页码:287 / 290
页数:4
相关论文
共 10 条
[1]   EFFECTS OF KAINIC ACID ON ION DISTRIBUTION AND ATP LEVELS OF STRIATAL SLICES INCUBATED INVITRO [J].
BIZIERE, K ;
COYLE, JT .
JOURNAL OF NEUROCHEMISTRY, 1978, 31 (02) :513-520
[2]   INFLUENCE OF CORTICO-STRIATAL AFFERENTS ON STRIATAL KAINIC ACID NEUROTOXICITY [J].
BIZIERE, K ;
COYLE, JT .
NEUROSCIENCE LETTERS, 1978, 8 (04) :303-310
[3]   LESION OF STRIATAL NEURONS WITH KAINIC ACID PROVIDES A MODEL FOR HUNTINGTONS-CHOREA [J].
COYLE, JT ;
SCHWARCZ, R .
NATURE, 1976, 263 (5574) :244-246
[4]   HIGH AFFINITY L-GLUTAMATE-H-3 BINDING TO POSTSYNAPTIC RECEPTOR-SITES ON RAT CEREBELLAR MEMBRANES [J].
FOSTER, AC ;
ROBERTS, PJ .
JOURNAL OF NEUROCHEMISTRY, 1978, 31 (06) :1467-1477
[5]   KAINIC ACID AND GLUTAMATE RECEPTOR [J].
HALL, JG ;
HICKS, TP ;
MCLENNAN, H .
NEUROSCIENCE LETTERS, 1978, 8 (02) :171-175
[6]   SELECTIVE DESTRUCTION OF NEURONS BY A TRANSMITTER AGONIST [J].
HERNDON, RM ;
COYLE, JT .
SCIENCE, 1977, 198 (4312) :71-72
[7]  
LONDON E, MOL PHARMACOL
[8]   KAINIC ACID - POWERFUL NEUROTOXIC ANALOG OF GLUTAMATE [J].
OLNEY, JW ;
RHEE, V ;
HO, OL .
BRAIN RESEARCH, 1974, 77 (03) :507-512
[9]   STRUCTURE-ACTIVITY RELATIONS FOR NEUROTOXICITY OF KAINIC ACID-DERIVATIVES AND GLUTAMATE ANALOGS [J].
SCHWARCZ, R ;
SCHOLZ, D ;
COYLE, JT .
NEUROPHARMACOLOGY, 1978, 17 (02) :145-151
[10]   POTENTIATION OF GLUTAMATE-INDUCED DEPOLARIZATION BY KAINIC ACID IN CRAYFISH OPENER MUSCLE [J].
SHINOZAK.H ;
SHIBUYA, I .
NEUROPHARMACOLOGY, 1974, 13 (10-1) :1057-1065