Knockout mice for pharmacological screening: testing the specificity of Na+-Ca2+ exchange inhibitors.

Abstract:

:The role of the Na+-Ca2+ exchanger as a major determinant of cell Ca2+ is well defined in cardiac tissue, and there has been much effort to develop specific inhibitors of the exchanger. We use a novel system to test the specificity of two putative specific inhibitors, KB-R7943 and SEA0400. The drugs are applied to electrically stimulated heart tubes from control mouse embryos or embryos with the Na+-Ca2+ exchanger knocked out. We monitored effects of the drugs on Ca2+ transients. Both drugs depress the Ca2+ transients at low concentrations even in the absence of any Na+-Ca2+ exchanger. KB-R7943 and SEA0400 are not completely specific and should be used with caution as Na+-Ca2+ exchange inhibitors.

journal_name

Circ Res

journal_title

Circulation research

authors

Reuter H,Henderson SA,Han T,Matsuda T,Baba A,Ross RS,Goldhaber JI,Philipson KD

doi

10.1161/01.res.0000027529.37429.38

subject

Has Abstract

pub_date

2002-07-26 00:00:00

pages

90-2

issue

2

eissn

0009-7330

issn

1524-4571

journal_volume

91

pub_type

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