Chloride channel inhibition by the venom of the scorpion Leiurus quinquestriatus.
The venom of the scorpion Leiurus quinquestriatus produced a significant, reversible inhibition of reconstituted Cl- channels of the small conductance type found in rat colonic epithelial cells. The kinetics of single-channel block by this venom were consistent with a first-order binding reaction in which the binding of one ligand molecule is sufficient to induce channel block. Single-channel mean block times were c.6 sec at -20 mV, and a KI in the submicromolar range is predicted. The active component has a mol. wt of roughly 5000 as judged by molecular sieve chromatography.
DeBin
J A
JA
Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA.
Strichartz
G R
GR
D000818:Animals; D001921:Brain / Q000201:enzymology; D001923:Brain Chemistry / Q000187:drug effects; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D002712:Chlorides / Q000378:metabolism*; D003106:Colon / Q000166:cytology / Q000378:metabolism; D004847:Epithelial Cells; D004848:Epithelium / Q000187:drug effects / Q000378:metabolism; D005260:Female; D007473:Ion Channels / Q000187:drug effects*; D007700:Kinetics; D008970:Molecular Weight; D011247:Pregnancy; D051381:Rats; D012604:Scorpion Venoms / Q000494:pharmacology*
D002712:Chlorides; D007473:Ion Channels; D012604:Scorpion Venoms