Direct inhibitory effects of an antisense oligodeoxynucleotide upon the volume-sensitive chloride current in rat osteoblast-like (ROS 17/2.8) cells.
The effects of a 15-mer antisense c-myc phosphorothioate modified oligodeoxynucleotide (OdN) upon the volume-sensitive Cl- current in ROS 17/2.8 cells were investigated using the whole-cell configuration of the patch clamp technique. At 5 microM, the OdN reversibly inhibited the current in a voltage- and time-dependent fashion. This was evident from the reduction in the peak current as assessed at the termination of each voltage pulse and an acceleration of the time-dependent inactivation present at strongly depolarised potentials. The kinetic modifications induced by the OdN suggest it may act by blocking the pore of open channels when the cell membrane potential is depolarised.
Gosling
M
M
Pharmaceutical Sciences Institute, Aston University, Birmingham, United Kingdom. m.gosling@cxwms.ac.uk
Akhtar
S
S
Smith
J W
JW
Poyner
D R
DR
D000818:Animals; D002460:Cell Line; D002712:Chlorides / Q000378:metabolism*; D008564:Membrane Potentials / Q000187:drug effects; D016376:Oligonucleotides, Antisense / Q000494:pharmacology*; D009994:Osmolar Concentration; D010006:Osteoblasts / Q000187:drug effects* / Q000378:metabolism; D016271:Proto-Oncogene Proteins c-myc / Q000235:genetics; D051381:Rats
D002712:Chlorides; D016376:Oligonucleotides, Antisense; D016271:Proto-Oncogene Proteins c-myc