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Blockade of Cl channels by organic and inorganic blockers in vascular smooth muscle cells by S. Kokubun; A. Saigusa; T. Tamura is a Medicine article available to read on EtoBox.

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The effects of C1 channel blockers on largeconductance (LC-type) C1 channels of cultured vascular smooth muscle cells (VSMC) were studied in order to characterize the channel pharmacologically. Intracellular disulphonic stilbene derivatives, such as 4,4'-diisothiocyanostilbene-2,2'-disulphonic acid (DIDS) and 4-acetamido-4-isothiocyanostilbene-2,2'-disulphonic acid (SITS) inhibited C1 channel activity in a dose-dependent manner. An obvious inhibitory effect of DIDS in this condition was obtained at concentrations higher than 5 gM, and the complete inhibition was obtained at around 100 gM, which was almost 10 times less than the effective dose of SITS. The inhibitory effect of DIDS was reversible at a drug concentration of lower than 50 gM. Single-channel conductance decreased as the concentration of DIDS increased. This decrease in the conductance was a consequence of unresolved openings of the channel due to fast blocking and unblocking rates of the drug. The C1 channel was also obviously inhibited by extracellular DIDS at a concentration of 1 mM. In addition, in cell-attached patches, 500 gM DIDS applied extracellularly inhibited C1 channel activated by the application of polymyx

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Author

S. Kokubun; A. Saigusa; T. Tamura

Publisher

Springer; Springer-Verlag; Springer Verlag; Springer Science and Business Media LLC (ISSN 0031-6768)

Published

1991

Language

EN

Field

Medicine (Life Sciences)