匹那地尔对兔肾动脉和肠系膜动脉舒张作用的比较。

A comparison of the relaxant effects of pinacidil in rabbit renal and mesenteric artery.

Gojković L, Kazić T

Department of Pharmacology, Medical Faculty, Belgrade, Yugoslavia.

Gen Pharmacol. 1994 Dec;25(8):1711-7. doi: 10.1016/0306-3623(94)90376-x.

Abstract

The relaxant effects of pinacidil were compared in isolated rabbit renal and mesenteric artery. 2. Pinacidil (10 nm-300 microM) relaxed renal and mesenteric arterial rings precontracted with phenylephrine with pD2 values of 5.11 +/- 0.03 and 6.27 +/- 0.04, respectively. 3. The inhibitory effect of pinacidil on the rabbit mesenteric artery was competitively antagonized by glibenclamide (1-10 microM). The calculated pKB value was 6.37 +/- 0.04. On the renal artery, glibenclamide (2-20 microM) did not significantly affect pinacidil-induced relaxation (P > 0.05). 4. Tetraethylammonium (TEA, 1-10 mM) competitively antagonized the pincaidil induced relaxation of the rabbit renal artery. The pKB value was 3.22 +/- 0.08. On the mesenteric artery TEA antagonized the effect of pinacidil in a noncompetitive manner. 5. The concentration-response curves for pinacidil on the rabbit renal and mesenteric artery were not affected by apamin (0.1 microM). 6. It is concluded that ATP-sensitive K+ channels (KATP) are not involved in pinacidil action on the rabbit renal artery. On the contrary, KATP are probably major sites of pinacidil action on the rabbit mesenteric artery.

摘要

比较了吡那地尔在离体兔肾动脉和肠系膜动脉中的舒张作用。2. 吡那地尔（10 nM - 300 μM）使预先用去氧肾上腺素预收缩的肾动脉和肠系膜动脉环舒张，其pD2值分别为5.11±0.03和6.27±0.04。3. 格列本脲（1 - 10 μM）竞争性拮抗吡那地尔对兔肠系膜动脉的抑制作用。计算得到的pKB值为6.37±0.04。在肾动脉上，格列本脲（2 - 20 μM）对吡那地尔诱导的舒张无显著影响（P>0.05）。4. 四乙铵（TEA，1 - 10 mM）竞争性拮抗吡那地尔诱导的兔肾动脉舒张。pKB值为3.22±0.08。在肠系膜动脉上，TEA以非竞争性方式拮抗吡那地尔的作用。5. 阿帕明（0.1 μM）不影响吡那地尔对兔肾动脉和肠系膜动脉的浓度 - 反应曲线。6. 得出结论：ATP敏感性钾通道（KATP）不参与吡那地尔对兔肾动脉的作用。相反，KATP可能是吡那地尔对兔肠系膜动脉作用的主要部位。