与硝苯地平、维拉帕米和地尔硫䓬相比，依福地平在体外对心肌和血管的作用。

Myocardial and vascular effects of efonidipine in vitro as compared with nifedipine, verapamil and diltiazem.

Tanaka H, Masumiya H, Sekine T, Sijuku T, Sugahara M, Taniguchi H, Terada M, Saito W, Shigenobu K

Department of Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.

Gen Pharmacol. 1996 Apr;27(3):451-4. doi: 10.1016/0306-3623(95)02065-9.

Abstract

Effects of efonidipine on isolated myocardial and aortic preparations were compared with those of nifedipine, verapamil and diltiazem. 2. All drugs produced concentration-dependent negative chronotropic effects on isolated guinea-pig atrial preparations. The potency order was efonidipine > or = nifedipine > diltiazem > or = verapamil, EC30 values being 3.08 x 10(-8)M, 3.48 x 10(-8)M, 1.27 x 10(-7)M and 1.47 x 10(-7)M, respectively. 3. Nifedipine, verapamil and diltiazem produced concentration-dependent negative inotropic effects on isolated guinea-pig left atrial preparations. The potency order was nifedipine > verapamil > diltiazem, EC30 values being 4.94 x 10(-8)M, 1.49 x 10(-7)M and 8.03 x 10(-7)M, respectively. Efonidipine, even at 1 microM produced no inotropic effect: 10 microM efonidipine decreased the contractile force by about 20%. 4. All drugs concentration-dependently attenuated the KCl-induced contraction of isolated rat aortic ring preparation. The potency order was nifedipine > efonidipine > verapamil > diltiazem, EC30 values being 2.98 x 10(-9)M, 1.24 x 10(-8)M, 3.96 x 10(-8)M and 2.13 x 10(-7)M, respectively. 5. Thus, efonidipine was demonstrated to be a potent vasodilator with negative chronotropic but minimal negative inotropic activity, which may be of benefit in the treatment of cardiovascular disorders.

摘要

将依福地平对离体心肌和主动脉制剂的作用与硝苯地平、维拉帕米和地尔硫䓬的作用进行了比较。2. 所有药物对离体豚鼠心房制剂均产生浓度依赖性负性变时作用。效价顺序为依福地平≥硝苯地平＞地尔硫䓬≥维拉帕米，EC30值分别为3.08×10⁻⁸M、3.48×10⁻⁸M、1.27×10⁻⁷M和1.47×10⁻⁷M。3. 硝苯地平、维拉帕米和地尔硫䓬对离体豚鼠左心房制剂产生浓度依赖性负性变力作用。效价顺序为硝苯地平＞维拉帕米＞地尔硫䓬，EC30值分别为4.94×10⁻⁸M、1.49×10⁻⁷M和8.03×10⁻⁷M。依福地平即使在1μM时也未产生变力作用：10μM依福地平使收缩力降低约20%。4. 所有药物均浓度依赖性地减弱氯化钾诱导的离体大鼠主动脉环制剂的收缩。效价顺序为硝苯地平＞依福地平＞维拉帕米＞地尔硫䓬，EC30值分别为2.98×10⁻⁹M、1.24×10⁻⁸M、3.96×10⁻⁸M和2.13×10⁻⁷M。5. 因此，依福地平被证明是一种强效血管扩张剂，具有负性变时作用但负性变力作用最小，这可能对心血管疾病的治疗有益。