[H-3] 7-OH-DPAT LABELS BOTH DOPAMINE-D3 RECEPTORS AND SIGMA-SITES IN THE BOVINE CAUDATE-NUCLEUS

被引:46
作者
SCHOEMAKER, H
机构
[1] Department of Preclinical Research, Synthélabo Recherche, 92220 Bagneux, 31, Avenue Paul Vaillant-Couturier
关键词
DOPAMINE-D3 RECEPTORS (BOVINE CAUDATE); 7-OH-DPAT; (7-HYDROXY-N; N-DI-N-PROPYL-2-AMINOTETRALIN); SIGMA-SITES;
D O I
10.1016/0014-2999(93)90259-K
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The binding of [H-3]7-hydroxy-N,N-di-n-propyl-2-aminotetralin (7-OH-DPAT) to membranes of the bovine caudate nucleus was characterized and shown to be heterogenous. While [H-3]7-OH-DPAT labels the dopamine D3 receptor in this tissue (K(i) = 4.8 nM), as shown by its sensitivity to dopamine and (-)-quinpirole, it also binds with high affinity (K(i) = 48 nM) to sigma recognition sites. The present results demonstrate that [H-3]7-OH-DPAT is a useful radioligand to label native D3 receptors in the bovine caudate, although care must be taken to assure its selectivity.
引用
收藏
页码:R1 / R2
页数:2
相关论文
共 8 条
[1]  
HACKSELL U, 1991, TXB DRUG DESIGN DEV, P26
[2]   INVITRO BINDING OF A NOVEL DOPAMINE-D(3) RECEPTOR LIGAND - [I-125] TRANS-7-OH-PIPAT-A [J].
KUNG, MP ;
KUNG, HF ;
CHUMPRADIT, S ;
FOULON, C .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1993, 235 (01) :165-166
[3]   DOPAMINE-D3 RECEPTOR MESSENGER-RNA AND BINDING-SITES IN HUMAN BRAIN [J].
LANDWEHRMEYER, B ;
MENGOD, G ;
PALACIOS, JM .
MOLECULAR BRAIN RESEARCH, 1993, 18 (1-2) :187-192
[4]   IDENTIFICATION, CHARACTERIZATION, AND LOCALIZATION OF THE DOPAMINE-D3 RECEPTOR IN RAT-BRAIN USING 7-[H-3]HYDROXY-N,N-DI-NORMAL-PROPYL-2-AMINOTETRALIN [J].
LEVESQUE, D ;
DIAZ, J ;
PILON, C ;
MARTRES, MP ;
GIROS, B ;
SOUIL, E ;
SCHOTT, D ;
MORGAT, JL ;
SCHWARTZ, JC ;
SOKOLOFF, P .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1992, 89 (17) :8155-8159
[5]   FURTHER INVITRO AND INVIVO STUDIES WITH THE PUTATIVE PRESYNAPTIC DOPAMINE AGONIST N,N-DIPROPYL-7-HYDROXY-2-AMINOTETRALIN [J].
MULDER, TBA ;
DEVRIES, JB ;
DIJKSTRA, D ;
WIECHERS, JW ;
GROL, CJ ;
HORN, AS .
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1987, 336 (05) :494-501
[6]   VISUALIZATION OF DOPAMINE-D(3)-LIKE RECEPTORS IN HUMAN BRAIN WITH [125I]EPIDEPRIDE [J].
MURRAY, AM ;
RYOO, H ;
JOYCE, JN .
EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1992, 227 (04) :443-445
[7]   MOLECULAR-CLONING AND CHARACTERIZATION OF A NOVEL DOPAMINE RECEPTOR (D3) AS A TARGET FOR NEUROLEPTICS [J].
SOKOLOFF, P ;
GIROS, B ;
MARTRES, MP ;
BOUTHENET, ML ;
SCHWARTZ, JC .
NATURE, 1990, 347 (6289) :146-151
[8]   PHARMACOLOGY OF HUMAN DOPAMINE D(3) RECEPTOR EXPRESSED IN A MAMMALIAN-CELL LINE - COMPARISON WITH D(2) RECEPTOR [J].
SOKOLOFF, P ;
ANDRIEUX, M ;
BESANCON, R ;
PILON, C ;
MARTRES, MP ;
GIROS, B ;
SCHWARTZ, JC .
EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1992, 225 (04) :331-337