蛋白激酶抑制剂H-7对5-羟色胺3型受体介导电流的抑制作用。
Inhibition of the 5-HT3 receptor-mediated current by the protein kinase inhibitor, H-7.
作者信息
Fan P
机构信息
Laboratory of Molecular and Cellular Neurobiology, National Institute on Alcohol Abuse and Alcoholism, Rockville, MD 20852.
出版信息
Brain Res. 1994 Jun 27;649(1-2):310-2. doi: 10.1016/0006-8993(94)91078-2.
PMID:7525009
Abstract
The effect of the protein kinase inhibitor, H-7, on the inward current mediated by 5-HT3 receptors was investigated with the whole-cell patch-clamp technique. H-7 inhibited the peak 5-HT current with an IC50 of 1.79 microM. The inhibition was quick, reversible and not blocked by the presence of 50 microM intracellular H-7. It is concluded that the effect of H-7 was independent of protein kinase activity.
摘要
采用全细胞膜片钳技术研究了蛋白激酶抑制剂H-7对5-羟色胺3（5-HT3）受体介导的内向电流的影响。H-7抑制5-HT电流峰值，其半数抑制浓度（IC50）为1.79微摩尔。这种抑制作用迅速、可逆，且不受细胞内50微摩尔H-7存在的阻断。得出的结论是，H-7的作用与蛋白激酶活性无关。
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