报道Ca2 +感光剂的影响利率的Ca2 +释放心肌肌钙蛋白C和troponin-tropomyosin复杂。

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史密斯SJ,英格兰PJ

报道Ca2 +感光剂的影响利率的Ca2 +释放心肌肌钙蛋白C和troponin-tropomyosin复杂。

Br J杂志。1990年8月,100 (4):779 - 85。

PubMed ID

2207500 (在PubMed

]

文摘

1。力生产的钙敏感性改变心肌纤维的某些药物。行动的网站三个这样的化合物(pimobendan、sulmazole isomazole)内的肌原纤维进行了研究。钙调素拮抗剂,perhexilene bepridil,已被证明改变贮藏寿命的钙依赖atp酶活性和oxmetidine的H2-receptor拮抗剂与钙调蛋白结合后,也进行了研究。2。钙的离解率从监管和高亲和力网站牛孤立心肌肌钙蛋白C (cTnC) stopped-flow荧光计测量。分离的速度是136.5 + / - 16 s - 1和1.3 + / - 0.20 s - 1(意思是+ / -东南部。意思是,n = 11决定;条件:100毫米氯化钾,10毫米拖把,MgCl2 3毫米,0.1毫米dithriothreitol, pH值7.0,15摄氏度),Sulmazole isomazole和perhexiline (50 microM)的最终浓度没有影响的Ca2 +离解率监管Ca2 +网站,表明这些化合物直接cTnC上不采取行动。3所示。Ca2 +的离解率监管网站略(大约20%)减少了pimobendan (50 - 100 microM)和有点增加oxmetidine (100 microM 28%)。 4. Bepridil (25 microM) reduced the rate of dissociation by 50%, indicating a direct effect of bepridil on TnC. 5. Sulmazole, isomazole, perhexiline, pimobendan (50 microM) and bepridil (25 microM) were without effect on the rate of dissociation of Ca2+ from the high affinity Ca2+/Mg2+ sites. Oxmetidine caused 24% decrease in the rate of Ca2+ dissociation from these sites. 6. The rate of dissociation of Ca2+ from the regulatory site on the complex of troponin-tropomyosin (TnTm) was measured. Sulmazole and pimobendan (50 microM) were without effect on the rate of dissociation of Ca2+ from the regulatory site in the protein complex, and isomazole (50 microM) caused only a slight reduction (23%). Perhexiline (50 microM) or bepridil (10 microM) reduced the rate of Ca2 dissociation by about 50%. The rate of dissociation of Ca2+ from the high affinity Ca2 +/Mg2 + sites was not altered by sulmazole, isomazole, or pimobendan (50 microM), but was decreased - 35% by perhexiline (50 microM) or bepridil (10 microM).

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药物靶点

药物	目标	类	生物	药理作用	行动
Bepridil	钠/ potassium-transporting atp酶亚基alpha -	蛋白质	人类	未知的	抑制剂	细节