摘要
采用基因克隆、膜片钳和微注射技术，分别将人的心律失常相关基因Ｋｖ１．５和Ｋｖ４．２ｃＤＮＡ转录为ｍＲＮＡ，然后将其分别注入蟾蜍卵母细胞（Ｘｅｎｏｐｕｓ Ｏｏｃｙｔｅｓ）上：在蟾蜍卵母细胞上分别获得纯净、单一的超速延迟性整流钾电流（Ｉｋｕｒ， ｕｌｔｒａｒａｐｉｄ ｄｅｌａｙｅｄ ｒｅｃｔｉｆｉｅｒ Ｋ＋ｃｕｒｒｅｎｔ）和瞬间外向钾电流（Ｉｔｏ，ｔｒａｎｓｉｅｎｔ ｏｕｔｗａｒｄ Ｋ＋ ｃｕｒｒｅｎｔ）表达，克服以往在筛选评价抗心律失常药物时，人新鲜心肌细胞取材困难、多种电流在细胞膜表面共同表达等缺点，从而建立评价Ⅲ类抗心律失常药物的先进药理模型，并筛选具有Ⅲ类抗心律失常药理作用的新化合物Ａ１９９８。
By techniques of gene clone, microinjection and patch-clamp, human arrhythmic related gene Kv1.5 and Kv4.2 are translated mRNA, and injected into Xenopus Oocytes, respectively. A pure and single K+ current of ultrarapid delayed rectifier K+ current (Ikur) or transient outward K+ current (Ito) is respectively expressed on Xenopus Oocytes. This is a moderm pharmasological model for evaluation class III antiarrhythmic drugs, overcomes many defects such as lacking human fresh cardiac muscle cells as material and co-expression of many currents on cell membrane. A new compound A1998 from Ocean material is evaluated in mis model for class III antiarrhythmic functions.
基金
九五"国家科技攻关<海洋生物活性物质>!(编号96-C02A14-01) The Project was supported by Foundation of "95"Science
关键词
心律失常基因
KV1.5
KV4.2
药理评价
arrhythmic related gene
Kv1.5
Kv4.2
Xenopus oocyte
gene clone
pharmacological evaluation
