Enantiomers of clofibric acid analogs have opposite actions on rat skeletal muscle chloride channels.
The S-(-) isomers of a series of clofibric acid analogs produced only a block of chloride conductance of rat skeletal muscle fibers with increasing concentrations until block was nearly complete. The R-(+) isomers, on the other hand, at low concentrations increased chloride conductance by as much as 9% to 39% and at higher concentrations decreased chloride conductance, but never by more than 27% of the control value. The actions of the enantiomeric pairs to either produce or inhibit myotonic excitability paralleled their ability to block or increase chloride conductance, respectively.
Conte-Camerino
D
D
Medicinal Chemistry Department, Faculty of Pharmacy, University of Bari, Italy.
Mambrini
M
M
DeLuca
A
A
Tricarico
D
D
Bryant
S H
SH
Tortorella
V
V
Bettoni
G
G
D000818:Animals; D002712:Chlorides / Q000378:metabolism*; D002994:Clofibrate / Q000031:analogs & derivatives*; D002995:Clofibric Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects*; D008297:Male; D009132:Muscles / Q000187:drug effects* / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D013237:Stereoisomerism
D002712:Chlorides; D007473:Ion Channels; D002995:Clofibric Acid; D002994:Clofibrate