IN-VIVO LABELING OF NICOTINIC CHOLINERGIC RECEPTORS IN BRAIN WITH [H-3] CYTISINE

被引:34
作者
FLESHER, JE
SCHEFFEL, U
LONDON, ED
FROST, JJ
机构
[1] JOHNS HOPKINS MED INST, DEPT RADIOL, BALTIMORE, MD 21287 USA
[2] NIDA, ADDICT RES CTR, BALTIMORE, MD 21224 USA
[3] UNIV MARYLAND, SCH MED, BALTIMORE, MD 21201 USA
关键词
H-3] CYTISINE; CENTRAL NICOTINIC CHOLINERGIC RECEPTORS; MOUSE BRAIN; IN VIVO BINDING;
D O I
10.1016/0024-3205(94)90146-5
中图分类号
R-3 [医学研究方法]; R3 [基础医学];
学科分类号
1001 ;
摘要
[H-3]Cytisine was evaluated as an in vivo ligand for the nicotinic cholinergic receptor (nAchR) in mouse brain. The tracer was injected intravenously, and radioactivity in brain regions was analyzed. Radioactivity peaked in the brain at 30 minutes. It was highest in the thalamus, intermediate in the superior colliculi, prefrontal cortex and hippocampus, and low in the cerebellum. Pretreatment with unlabeled cytisine inhibited binding in the thalamus, but not in the cerebellum. Binding was displaced by 1-nicotine, but not by d-nicotine or dexetimide. The results suggest that cytisine, appropriately labeled with a positron emitting radionuclide, may be useful for study of nicotinic cholinergic receptors in humans by emission computed tomography.
引用
收藏
页码:1883 / 1890
页数:8
相关论文
共 24 条
[1]   INVIVO SPECIFIC BINDING OF [H-3] 1-NICOTINE IN THE MOUSE-BRAIN [J].
BROUSSOLLE, EP ;
WONG, DF ;
FANELLI, RJ ;
LONDON, ED .
LIFE SCIENCES, 1989, 44 (16) :1123-1132
[2]   AUTORADIOGRAPHIC DISTRIBUTION OF NICOTINE RECEPTORS IN RAT-BRAIN [J].
CLARKE, PBS ;
PERT, CB ;
PERT, A .
BRAIN RESEARCH, 1984, 323 (02) :390-395
[3]  
CLARKE PBS, 1985, J NEUROSCI, V5, P1307
[4]   H-3 DIPRENORPHINE IS SELECTIVE FOR MU-OPIATE RECEPTORS INVIVO [J].
FROST, JJ ;
SMITH, AC ;
WAGNER, HN .
LIFE SCIENCES, 1986, 38 (17) :1597-1606
[5]  
FROST JJ, 1987, LIFE SCI, V40, P987
[6]  
HENNINGFIELD JE, 1984, ADV BEHAV PHARMACOL, V4, P131
[7]   MUSCARINIC AND NICOTINIC CHOLINERGIC BINDING-SITES IN ALZHEIMERS-DISEASE CEREBRAL-CORTEX [J].
KELLAR, KJ ;
WHITEHOUSE, PJ ;
MARTINOBARROWS, AM ;
MARCUS, K ;
PRICE, DL .
BRAIN RESEARCH, 1987, 436 (01) :62-68
[8]   STEREOSPECIFIC INVITRO BINDING OF [DEXETIMIDE-H-3 TO BRAIN MUSCARINIC RECEPTORS [J].
LADURON, PM ;
VERWIMP, M ;
LEYSEN, JE .
JOURNAL OF NEUROCHEMISTRY, 1979, 32 (02) :421-427
[9]   COMPARATIVE-ANALYSIS OF NICOTINE-LIKE RECEPTOR LIGAND INTERACTIONS IN RODENT BRAIN HOMOGENATE [J].
LARSSON, C ;
NORDBERG, A .
JOURNAL OF NEUROCHEMISTRY, 1985, 45 (01) :24-31
[10]   AUTORADIOGRAPHIC LOCALIZATION OF [H-3] NICOTINE BINDING-SITES IN THE RAT-BRAIN [J].
LONDON, ED ;
WALLER, SB ;
WAMSLEY, JK .
NEUROSCIENCE LETTERS, 1985, 53 (02) :179-184