The human dopamine D2Longer receptor has a high-affinity state and inhibits adenylyl cyclase

被引：25

作者：

Liu, ISC

George, SR

Seeman, P

机构：

[1] Univ Toronto, Dept Pharmacol, Toronto, ON M5S 1A8, Canada

[2] Univ Toronto, Dept Psychiat, Toronto, ON M5S 1A8, Canada

[3] Univ Toronto, Dept Med, Toronto, ON M5S 1A8, Canada

来源：

MOLECULAR BRAIN RESEARCH | 2000年 / 77卷 / 02期

基金：

英国医学研究理事会;

关键词：

dopamine receptor; D2 splice variant; D2; mRNA; D2(Longer); psychosis;

D O I：

10.1016/S0169-328X(00)00064-4

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

Brain dopamine D2 receptors are the main targets for antipsychotic and anti-Parkinsonian drugs. The dopamine D2 receptor has three forms, D2(Short), D2(Long) and D2(Longer), D2(Longer) is a newly found splice variant which contains two additional amino acids (valine and glutamine) in the third cytoplasmic loop of the receptor. To determine whether D2(Longer) was functional, the cDNA was transfected into CHO cells. D2(Longer) revealed a high-affinity state for dopamine (similar to 1.5 nM), and mediated dopamine-inhibited adenylyl cyclase. (C) 2000 Elsevier Science B.V. All rights reserved.

引用

收藏

页码：281 / 284

页数：4

相关论文

共 18 条

[1] CLONING AND EXPRESSION OF A RAT D2 DOPAMINE RECEPTOR CDNA [J].

BUNZOW, JR ;

VANTOL, HHM ;

GRANDY, DK ;

ALBERT, P ;

SALON, J ;

CHRISTIE, MJ ;

MACHIDA, CA ;

NEVE, KA ;

CIVELLI, O .

NATURE, 1988, 336 (6201) :783-787

[2] THE FUNCTIONAL-STATE OF THE DOPAMINE RECEPTOR IN THE ANTERIOR-PITUITARY IS IN THE HIGH-AFFINITY FORM [J].

GEORGE, SR ;

WATANABE, M ;

DIPAOLO, T ;

FALARDEAU, P ;

LABRIE, F ;

SEEMAN, P .

ENDOCRINOLOGY, 1985, 117 (02) :690-697

[3] ALTERNATIVE SPLICING DIRECTS THE EXPRESSION OF 2 D2 DOPAMINE RECEPTOR ISOFORMS [J].

GIROS, B ;

SOKOLOFF, P ;

MARTRES, MP ;

RIOU, JF ;

EMORINE, LJ ;

SCHWARTZ, JC .

NATURE, 1989, 342 (6252) :923-926

[4] [H-3] DOMPERIDONE LABELS ONLY A SINGLE POPULATION OF RECEPTORS WHICH CONVERT FROM HIGH TO LOW AFFINITY FOR DOPAMINE IN RAT-BRAIN [J].

GRIGORIADIS, D ;

SEEMAN, P .

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1986, 332 (01) :21-25

[5] [H-3]DOPAMINE LABELING OF D3 DOPAMINERGIC SITES IN HUMAN, RAT, AND CALF BRAIN [J].

LIST, SJ ;

SEEMAN, P .

JOURNAL OF NEUROCHEMISTRY, 1982, 39 (05) :1363-1373

[6]

Liu ISC, 1996, AM J MED GENET, V61, P277, DOI 10.1002/(SICI)1096-8628(19960122)61:3<277::AID-AJMG14>3.0.CO

[7]

2-Q

[8] MULTIPLE D2 DOPAMINE-RECEPTORS PRODUCED BY ALTERNATIVE RNA SPLICING [J].

MONSMA, FJ ;

MCVITTIE, LD ;

GERFEN, CR ;

MAHAN, LC ;

SIBLEY, DR .

NATURE, 1989, 342 (6252) :926-929

[9] LIGAND - A VERSATILE COMPUTERIZED APPROACH FOR CHARACTERIZATION OF LIGAND-BINDING SYSTEMS [J].

MUNSON, PJ ;

RODBARD, D .

ANALYTICAL BIOCHEMISTRY, 1980, 107 (01) :220-239

[10] Resistance of the dopamine D2(L) receptor to desensitization accompanies the up-regulation of receptors on to the surface of Sf9 cells [J].

Ng, GYK ;

Varghese, G ;

Chung, HT ;

Trogadis, J ;

Seeman, P ;

ODowd, BF ;

George, SR .

ENDOCRINOLOGY, 1997, 138 (10) :4199-4206