Jovanović A, Gojković L J, Kazić T, Grbović L, Tulić I
Department of Pharmacology, Medical Faculty, Belgrade, Yugoslavia.
Arch Int Pharmacodyn Ther. 1994 May-Jun;327(3):344-54.
The effect of pinacidil on human isolated uterine artery rings was investigated. Pinacidil (10 nM-300 microM) induced a concentration-dependent relaxation of the precontracted arterial segments (pD2: 6.26; maximal response: 98.5%). Apamin (1 microM) and tetraethylammonium (6 mM) had no effects on the pinacidil-evoked relaxation, while 4-aminopyridine (0.1-6 mM) and glibenclamide (1-10 microM) competitively antagonized the response to pinacidil. The dissociation constants for 4-aminopyridine and glibenclamide were 240 microM and 0.40 microM, respectively. It is concluded that, in human uterine arteries, pinacidil induces relaxation. On the basis of differential antagonist affinities, we suggest that pinacidil produces a relaxation of this blood vessel through activation of glibenclamide-sensitive, ATP-dependent potassium channels.
研究了吡那地尔对人离体子宫动脉环的作用。吡那地尔（10 nM - 300 μM）可使预收缩的动脉段产生浓度依赖性舒张（pD2：6.26；最大反应：98.5%）。蜂毒明肽（1 μM）和四乙铵（6 mM）对吡那地尔引起的舒张无影响，而4 - 氨基吡啶（0.1 - 6 mM）和格列本脲（1 - 10 μM）竞争性拮抗对吡那地尔的反应。4 - 氨基吡啶和格列本脲的解离常数分别为240 μM和0.40 μM。结论是，在人子宫动脉中，吡那地尔可诱导舒张。基于不同拮抗剂的亲和力，我们认为吡那地尔通过激活格列本脲敏感的、ATP依赖性钾通道使该血管产生舒张。
