Posner P, Chiou C Y
Pharmacology. 1976;14(2):97-103. doi: 10.1159/000136585.
The agent, 6-(N,N-diethylamino)-hexyl- 3, 4, 5,-Trimethoxybenzoate (TMB-6) which relaxes smooth and skeletal muscle by interfering with intracellular Ca ++ availability was tested for its electrophysiological effects on canine cardiac Purkinje fibres and feline papillary muscles. In both tissues the drug causes a decrease in resting membrane potential and action potential amplitude as well as spontaneous rate in Purkinje fibres, and an increase in stimulus needed to reach threshold. The minimum effective dose for both tissues was similar at 7.32 x 10-5 M. The drug effects were reversible in both tissues upon removal of the TMB-6. The Ca++ -dependent action potentials of canine cardiac Purkinje fibres were also inhibited by TMB-6 at dose range of 7.32 x 10-5 -24.4 x 10-5 M. Because of its electro physiological effects of threshold, automaticity and "slow response" action potentials and its reversibility, TMB-6 could become a useful antiarrhythmic drug.
药物6-(N,N-二乙氨基)-己基-3,4,5-三甲氧基苯甲酸酯(TMB-6)通过干扰细胞内钙离子的可用性来舒张平滑肌和骨骼肌,该药物对犬心脏浦肯野纤维和猫乳头肌的电生理效应进行了测试。在这两种组织中,该药物都会导致静息膜电位和动作电位幅度降低,以及浦肯野纤维的自发频率降低,并增加达到阈值所需的刺激。两种组织的最小有效剂量相似,为7.32×10-5M。去除TMB-6后,两种组织中的药物效应都是可逆的。在7.32×10-5 - 24.4×10-5M的剂量范围内,TMB-6也会抑制犬心脏浦肯野纤维的钙依赖性动作电位。由于其对阈值、自律性和“慢反应”动作电位的电生理效应及其可逆性,TMB-6可能成为一种有用的抗心律失常药物。