Noguchi K, Takahashi K, Kaneko K, Higuchi S
Pharmacology Laboratory, Pharmaceutical Research Laboratories, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.
Arzneimittelforschung. 1998 Jan;48(1):22-5.
The effects of LU49700 (CAS 116759-60-5), the main metabolite of gallopamil (CAS 16662-47-8) on the mechanical response of isolated rat aortic and guinea-pig ventricular papillary muscle preparations were compared with those of gallopamil. Gallopamil and LU49700 inhibited the 64 mmol/l KCl-induced contraction of rat aorta in a concentration-dependent manner. The vasorelaxant potency of LU49700 was 244 times weaker than that of gallopamil. Gallopamil and LU49700 produced concentration-dependent negative inotropic effects on isolated right ventricular papillary muscles. The negative inotropic potency of LU49700 was 418 times weaker than that of gallopamil. These findings indicate that LU49700 has a weaker cardiovascular depressant potency than gallopamil. Therefore, LU49700 may not mediate the effects of gallopamil for treating subjects with cardiovascular diseases.
将加洛帕米（CAS 16662-47-8）的主要代谢物LU49700（CAS 116759-60-5）对离体大鼠主动脉和豚鼠心室乳头肌标本机械反应的影响与加洛帕米的影响进行了比较。加洛帕米和LU49700以浓度依赖性方式抑制64 mmol/l氯化钾诱导的大鼠主动脉收缩。LU49700的血管舒张效力比加洛帕米弱244倍。加洛帕米和LU49700对离体右心室乳头肌产生浓度依赖性负性肌力作用。LU49700的负性肌力效力比加洛帕米弱418倍。这些发现表明，LU49700的心血管抑制效力比加洛帕米弱。因此，LU49700可能不介导加洛帕米治疗心血管疾病患者的作用。
