Reversible blockade of the calcium-activated nonselective cation channel in brown fat cells by the sulfhydryl reagents mercury and thimerosal.

ABSTRACT

We have used patch-clamp techniques to study the effect of the sulfhydryl group oxidizing agents mercury and thimerosal on calcium-activated nonselective cation channels from brown adipose tissue. 100 nmol/l mercury and 50 mumol/l thimerosal induced a complete block. Blockade could be reversed by reduction of the mercaptide by dithiotreitol (DTT). Mercury was found to be the most potent blocker (IC50-value 21 x 10(-9) mol/l), whereas thimerosal (IC50-value 1.5 x 10(-6) mol/l) was as effective as 3',5-dichlorodiphenylamine-2-carboxylic acid (DCDPC). The DCDPC effect, however, could not be reversed by DTT, indicating different blocking mechanisms. It is concluded that SH-groups are involved in gating of the calcium-activated nonselective channel.