摘要
目的阐明AMP579与腺苷不同药理作用与临床效果的机制。方法采用全细胞膜片钳记录Na+/Ca2 +交换电流。结果AMP579对Na+/Ca2 +交换的外向和内向电流均呈浓度依赖性增强。灌流腺苷A1受体阻断剂PD116948 30μmol·L-1,A2受体阻断剂DMPX10μmol·L-1,蛋白激酶A特异阻断剂KT5720 0 .2μmol·L-1或蛋白激酶C特异阻断剂GF109203X0 .4μmol·L-1对AMP579 Na+/Ca2 +交换电流的激动作用均无影响,提示AMP579对Na+/Ca2 +交换电流具有直接的激动作用。结论AMP579对Na+/Ca2 +交换电流可能具有直接的激动作用。
AIM To elucidate possible mechanisms underlying the differences between 1 S-[1 a, 2b, 3b, 4a （ S＊ ）]-4-[ 7-I[ 1-（ 3-chloro-2-thienyl ） methylpmpyl ] pmpyl-amino ]-3H-imidazo [ 4, 5-b ] pyridyl-3-yl]-N- ethyl-2, 3-dihydroxycyclopentane carboxamide （ AMP- 579） and adenosine in pharmacological and clinical effects. METHODS Na^＋/Ca^2＋ exchange current was recorded by patch-clamp technique in whole-cell cortfiguration. RESULTS AMP579 significantly enhanced both outward and inward Na^＋/Ca^2＋ exchange currents in a concentration dependent manner. Neither infusion of an adenosine Al receptor antagonist PD116948 30μmol· L^-1 or an adenosine A2 receptor antagonist DMPX 10μmol· L^-1 nor a protein kinase A special blocker KT 5720 0.2μmol· L^-1 or a protein kinase C special blocker GF 109203X 0. 4 μmol· L^-1 had effect on Na^＋/Ca^2＋ exchange current increased by AMP579, suggesting that AMP579 possess a direct activating effect on Na^＋/Ca^2＋ exchange possesses current. current a direct CONCLUSION AMP579 possibly activating effect on Na^＋/Ca^2＋ exchange current.
出处
《中国药理学与毒理学杂志》
CAS
CSCD
北大核心
2005年第4期254-258,共5页
Chinese Journal of Pharmacology and Toxicology
关键词
AMP579
心肌
腺苷
钠/钙交换电流
膜片钳技术
全细胞
AMP579
myocardium
adenosine
sodium/calcium exchange current
patch clamp technique, wholecell
