van Meel J C
Department of Cardiovascular Research, Dr. Karl Thomae GmbH, Biberach an der Riss, Fed. Rep. of Germany.
Arzneimittelforschung. 1987 Jun;37(6):679-82.
Nine cardiotonics of different chemical structure were investigated on their ability to influence calcium-induced isometric contractions of chemically skinned porcine myocardial fibers. It was found that at a concentration of 10(-4) mol/l amrinone, enoximone, imazodan, milrinone, piperanometozine and piroximone were without effect on calcium-induced tension development of skinned fibers. 3-Amino-6-methyl-5-phenyl-2(1H)-pyridinone (APP), pimobendan and sulmazole enhanced the isometric contractions induced by 0.66 mumol/l Ca++ concentration-dependently. The intrinsic activity of pimobendan was much higher than for sulmazole or APP. Comparing equieffective concentrations inducing 35% additional tension development, the rank order of potency was: pimobendan greater than APP greater than sulmazole.
研究了九种不同化学结构的强心剂对化学去表皮猪心肌纤维钙诱导等长收缩的影响能力。结果发现，在浓度为10(-4)mol/l时，氨力农、依诺昔酮、咪唑旦、米力农、哌拉诺美嗪和吡罗昔酮对去表皮纤维的钙诱导张力发展没有影响。3-氨基-6-甲基-5-苯基-2(1H)-吡啶酮（APP）、匹莫苯丹和舒马唑以浓度依赖的方式增强了由0.66μmol/l Ca++诱导的等长收缩。匹莫苯丹的内在活性远高于舒马唑或APP。比较诱导额外35%张力发展的等效浓度，效价顺序为：匹莫苯丹＞APP＞舒马唑。
