Nakamura Y, Shiraki Y, Nabata H, Sakai K
Jpn J Pharmacol. 1984 Mar;34(3):269-76. doi: 10.1254/jjp.34.269.
The effects of nicorandil (NCR) on tracheal and vascular smooth muscle in the dog were compared with those of nitroglycerin (NTG) in in vitro and in vivo preparations. In the isolated tracheal strip and coronary artery preparations contracted with KCl (30 mM), the ability of NCR to relax these muscles and arteries by 50% was 1/10-1/15 as potent as NTG. In blood-perfused tracheal preparations, single doses of NCR and NTG injected into the tracheal artery produced dose-related decreases in the intraluminal pressure (ILP) of the trachea (relaxation) and increases in the tracheal blood flow (TBF). When the potency of NCR relative to that of NTG was compared on the basis of doses decreasing the ILP and increasing the TBF by 50%, NCR was 822 times less potent than NTG in producing tracheal relaxation and 572 times less potent in producing tracheal vasodilation. The effects of NCR on the ILP and TBF were not antagonized by propranolol. In non-perfused tracheal preparations, the two drugs administered i.v. elicited the effects in a similar dose-dependent manner; decreases in systemic blood pressure (SBP), left ventricular systolic pressure (LVP), pressure-rate product (PRP), femoral vascular resistance (FVR), and ILP and increases in heart rate (HR) and LVdP/dt max. The results show that NCR has a potent bronchodilating action and that its pharmacological profile is somewhat similar to NTG.
在体外和体内实验中，比较了尼可地尔（NCR）与硝酸甘油（NTG）对犬气管和血管平滑肌的作用。在氯化钾（30 mM）收缩的离体气管条和冠状动脉制剂中，NCR使这些肌肉和动脉松弛50%的能力仅为NTG的1/10 - 1/15。在血液灌注的气管制剂中，向气管动脉注射单剂量的NCR和NTG会使气管腔内压力（ILP）呈剂量依赖性降低（松弛），并使气管血流量（TBF）增加。当根据使ILP降低和TBF增加50%的剂量来比较NCR相对于NTG的效力时，NCR产生气管松弛的效力比NTG低822倍，并使气管血管舒张的效力低572倍。NCR对ILP和TBF的作用不受普萘洛尔的拮抗。在非灌注气管制剂中，静脉注射这两种药物会以相似的剂量依赖性方式产生作用；使全身血压（SBP）、左心室收缩压（LVP）、压力 - 心率乘积（PRP）、股血管阻力（FVR）和ILP降低，并使心率（HR）和左心室dp/dt max增加。结果表明，NCR具有强大的支气管舒张作用，其药理学特征与NTG有些相似。
