[3H]β-CIT:: a radioligand for dopamine transporters in rat brain tissue

被引：42

作者：

Kula, NS

Baldessarini, RJ

Tarazi, FI

Fisser, R

Wang, SY

Trometer, J

Neumeyer, JL

机构：

[1] Massachusetts Gen Hosp, McLean Div, Mailman Res Ctr, Belmont, MA 02478 USA

[2] Massachusetts Gen Hosp, McLean Div, Addict Res Ctr, Belmont, MA 02478 USA

[3] Harvard Univ, Sch Med, Consolidated Dept Psychiat, Boston, MA USA

[4] Harvard Univ, Sch Med, Neurosci Program, Boston, MA 02115 USA

[5] Res Biochem Int, Natick, MA USA

[6] New England Nucl, Boston, MA USA

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1999年 / 385卷 / 2-3期

关键词：

autoradiography; H-3]beta-CIT; dopamine; monoamine; transporter; tropane;

D O I：

10.1016/S0014-2999(99)00695-0

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

[H-3]2-beta-carbomethoxy-3-beta-[4'-iodophenyl]tropane (beta-CIT) was prepared and evaluated. With rat forebrain tissue, [H-3]beta-CIT showed high affinity for dopamine transporters (DAT), with selectivity for DAT over norepinephrine transporters, but not serotonin transporters, as well as DAT-stereoselectivity with beta-CIT, amphetamine and methylphenidate. Affinity and selectivity for 53 compounds assayed with [H-3]beta-CIT and standard DAT radioligand [H-3]GBR-12935 were highly correlated (r > 0.95). [H-3]beta-CIT is proposed as a useful, high-affinity DAT radioprobe. (C) 1999 Elsevier Science B.V. All rights reserved.

引用

页码：291 / 294

页数：4

共 16 条

[1] BIOCHEMICAL AND PHARMACOLOGICAL CHARACTERIZATION OF [H-3] GBR-12935 BINDING INVITRO TO RAT STRIATAL MEMBRANES - LABELING OF THE DOPAMINE UPTAKE COMPLEX [J].