CHLORIDE CHANNEL INHIBITION BY THE VENOM OF THE SCORPION LEIURUS-QUINQUESTRIATUS

被引:97
作者
DEBIN, JA
STRICHARTZ, GR
机构
[1] HARVARD UNIV,SCH MED,DEPT BIOL CHEM & MOLEC PHARMACOL,BOSTON,MA 02115
[2] BRIGHAM & WOMENS HOSP,BENJAMIN COVINO LABS ANESTHESIA RES,BOSTON,MA 02115
关键词
D O I
10.1016/0041-0101(91)90128-E
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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 K1 in the submicromolar range is predicted. The active component has a mol. wt of roughly 5000 as judged by molecular sieve chromatography.
引用
收藏
页码:1403 / 1408
页数:6
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