绑定的K (ATP)通道调节器在大鼠心脏膜。

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Loffler-Walz C, Quast U

绑定的K (ATP)通道调节器在大鼠心脏膜。

Br J杂志。1998年4月,123 (7):1395 - 402。

PubMed ID

9579735 (在PubMed

]

文摘

1。[3 h] -P1075的绑定,一个强有力的揭幕战的腺苷三磷酸(ATP)——敏感的K +通道,研究了原油的心膜制备的老鼠,在37度2。绑定需要MgATP。存在一个ATP-regenerating系统,MgATP支持[3 h] -P1075绑定的EC50值100 microM和希尔系数为1.4。3所示。在饱和实验[3 h] -P1075绑定与KD值均匀6 + / 1 nM和绑定能力(Bmax) 33 + / 3 fmol毫克(1)蛋白质。4所示。在添加过多的未标记的P1075, [3 h] -P1075-receptor复杂分离mono-exponential地离解速率常数为0.13 + / - -0.01分钟(1)。如果bi-molecular协会机制认为,依赖标签集中了协会的协会动力学速率常数为0.030 + / - -0.003海里(1)最小(1)。从动力学实验KD值被计算为4.7 + / - -0.6海里。 5. Openers of the ATP-sensitive K+ channel belonging to different structural classes inhibited specific [3H]-P1075 binding in a monophasic manner to completion; an exception was minoxidil sulphate where maximum inhibition was 68%. The potencies of the openers in this assay agree with published values obtained in rat cardiocytes and are on average 3.5 times lower than those determined in rat aorta. 6. Sulphonylureas, such as glibenclamide and glibornuride and the sulphonylurea-related carboxylate, AZ-DF 265, inhibited [3H]-P1075 binding with biphasic inhibition curves. The high affinity component comprised about 60% of the curves with the IC50 value of glibenclamide being approximately 90 nM; affinities for the low affinity component were in the microM concentration range. The fluorescein derivative, phloxine B, showed a monophasic inhibition curve with an IC50 value of 6 microM, a maximum inhibition of 94% and a Hill coefficient of 1.5. 7. It is concluded that binding studies with [3H]-P1075 are feasible in rat heart membranes in the presence of MgATP and of an ATP-regenerating system. The pharmacological profile of the [3H]-P1075 binding sites in the cardiac preparation, which probably contains sulphonylurea receptors (SURs) from cardiac myocytes (SUR2A) and vascular smooth muscle cells (SUR2B), differs from that expected for SUR2A and SUR2B.

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药物靶点

药物	目标	类	生物	药理作用	行动
米诺地尔	ATP-sensitive内向整流钾通道1	蛋白质	人类	是的	诱导物	细节