EVIDENCE THAT STRIATAL SYNTHESIS-INHIBITING AUTORECEPTORS ARE DOPAMINE-D(3) RECEPTORS

被引：92

作者：

MELLER, E ^{[1
]}

BOHMAKER, K ^{[1
]}

GOLDSTEIN, M ^{[1
]}

BASHAM, DA ^{[1
]}

机构：

[1] NYU,SCH MED,DEPT PSYCHIAT,NEUROCHEM RES LABS,NEW YORK,NY 10016

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1993年 / 249卷 / 01期

关键词：

DOPAMINE-D(3) RECEPTOR; DOPAMINE-D(2) RECEPTOR; STRIATAL DOPAMINE AUTORECEPTOR;

D O I：

10.1016/0014-2999(93)90674-7

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The activation constants (K(A); dose required to occupy 50% of receptors) for reversal of gamma-butyrolactone (GBL)-induced elevation of striatal L-3,4-dihydroxyphenylalanine (L-DOPA) levels via stimulation of presynaptic dopamine receptors were determined for apomorphine and two dopamine D3 receptor-selective agonists, quinpirole and LY163502 (quinelorane). The K(A) values correlated significantly with the affinities (K(i)) of the agonists for the D3 (r = 0.999, P < 0.05) but not the D2 (r = - 0. 13) receptor, suggesting that striatal synthesis-inhibiting autoreceptors are of the D3 rather than the D2 subtype.

引用

页码：R5 / R6

页数：2

共 8 条

[1]

BOUNDY VA, 1993, J PHARMACOL EXP THER, V264, P1002

[2] MODULATION OF COCAINE SELF-ADMINISTRATION IN THE RAT THROUGH D-3 DOPAMINE-RECEPTORS [J].

CAINE, SB ;

KOOB, GF .

SCIENCE, 1993, 260 (5115) :1814-1816

[3] MOLECULAR DIVERSITY OF THE DOPAMINE-RECEPTORS [J].

CIVELLI, O ;

BUNZOW, JR ;

GRANDY, DK .

ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, 1993, 33 :281-307

[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]

MELLER E, 1987, MOL PHARMACOL, V31, P592

[6] IMPORTANT CONCEPTS OF RECEPTOR THEORY [J].

RUFFOLO, RR .

JOURNAL OF AUTONOMIC PHARMACOLOGY, 1982, 2 (04) :277-295

[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

← 1 →