RADIO-LABELING AND FLUORESCENCE-LABELING OF THAPSIGARGIN, A SELECTIVE INHIBITOR OF MICROSOMAL CALCIUM-ATPASE

被引：6

作者：

ANDERSEN, A ^{[1
]}

LAURIDSEN, A ^{[1
]}

CHRISTENSEN, SB ^{[1
]}

机构：

[1] PHARMABIOTEC,ROYAL DANISH SCH PHARM,DEPT ORGAN CHEM,UNIVERSITETSPARKEN 2,DK-2100 COPENHAGEN 0,DENMARK

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1992年 / 31卷 / 03期

关键词：

THAPSIGARGIN; CALCIUM-ATPASE; DEUTERIUM; TRITIUM; FLUORESCENCE; DANSYL;

D O I：

10.1002/jlcr.2580310305

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Debutanoylthapsigargin (2) labelled in the skeleton was prepared by stereoselective reduction of the ketone (3) obtained by oxidation of debutanoylthapsigargin. Butanoylation of 2 yielded thapsigargin 1. The use of sodium boro[H-3]hydride as a reducing agent afforded labelled debutanoylthapsigargin with a specific activity of 22 Ci/mmol. A fluorescent analogue of thapsigargin (4a) was prepared by allowing 2 to react with N-dansyl-beta-alanine. Acetylation of 4a afforded a trisacetate (4c) the missing bioactivity of which allows it to be used as a negative control.

引用

页码：199 / 206

页数：8

共 14 条

[1] THE ABILITY OF THAPSIGARGIN AND THAPSIGARGICIN TO ACTIVATE CELLS INVOLVED IN THE INFLAMMATORY RESPONSE [J].