匹那地尔可打开钾离子选择性通道，导致大鼠肠系膜阻力血管超极化并使去甲肾上腺素引起的收缩舒张。
Pinacidil opens K+-selective channels causing hyperpolarization and relaxation of noradrenaline contractions in rat mesenteric resistance vessels.
作者信息
Videbaek L M, Aalkjaer C, Mulvany M J
机构信息
Biophysics Institute, Aarhus University, Denmark.
出版信息
Br J Pharmacol. 1988 Sep;95(1):103-8. doi: 10.1111/j.1476-5381.1988.tb16553.x.
Abstract
- The effects of pinacidil on noradrenaline-induced tone, smooth muscle membrane potential and 42K- and 86Rb-efflux from isolated mesenteric resistance vessels (internal diameter 200 microns) of the rat have been studied. 2. Pinacidil (0.3-10 microM) produced concentration-dependent suppression of noradrenaline-induced tone. 3. Pinacidil (0.3-10 microM) caused concentration-dependent hyperpolarization of the smooth muscle. 4. In rat resistance vessels loaded with 42K, pinacidil (1-10 microM) significantly increased the 42K-efflux rate constant. 5. With the use of 86Rb as a marker for K+, 1 microM pinacidil did not affect the 86Rb-efflux rate constant, while 10 microM pinacidil transiently increased the 86Rb rate constant. 6. The results indicate that the relaxant action of pinacidil in these vessels is due to the opening of K+-channels and consequent hyperpolarization. The K+-channels opened are selective for 42K over 86Rb.
摘要
- 研究了吡那地尔对去甲肾上腺素引起的张力、平滑肌膜电位以及大鼠离体肠系膜阻力血管（内径200微米）中42K和86Rb外流的影响。2. 吡那地尔（0.3 - 10微摩尔）对去甲肾上腺素引起的张力产生浓度依赖性抑制。3. 吡那地尔（0.3 - 10微摩尔）引起平滑肌浓度依赖性超极化。4. 在加载42K的大鼠阻力血管中，吡那地尔（1 - 10微摩尔）显著增加42K外流速率常数。5. 以86Rb作为K+的标记物，1微摩尔吡那地尔不影响86Rb外流速率常数，而10微摩尔吡那地尔短暂增加86Rb速率常数。6. 结果表明，吡那地尔在这些血管中的舒张作用是由于K+通道开放及随之而来的超极化。开放的K+通道对42K的选择性高于86Rb。
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