SYNTHESIS OF [H-3] DIPPA - A POTENT IRREVERSIBLE ANTAGONIST SELECTIVE FOR THE KAPPA-OPIOID RECEPTOR

被引：2
作者：
CHANG, AC
TROMETER, JD
PORTOGHESE, PS
机构：
[1] UNIV MINNESOTA,COLL PHARM,DEPT MED CHEM,MINNEAPOLIS,MN 55455
[2] DUPONT CO INC,DEPT MED PROD,BOSTON,MA 02118
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1995年 / 36卷 / 06期
关键词：
DIPPA; ANTAGONIST; KAPPA; RADIOLABELED; AFFINITY LABEL; TRITIUM;
D O I：
10.1002/jlcr.2580360607
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]acetamide (1, DIPPA) has been previously reported to be an opioid receptor affinity label that produces selective and long-lasting kappa opioid receptor antagonism in mice. High specific activity [H-3]DIPPA (39.7 Ci/mmol) was prepared by bromination and catalytic tritiation of the amino precursor of DIPPA followed by conversion to the isothiocyanate with thiophosgene.
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页码：553 / 557
页数：5
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