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本文观察噻吗心安(5×10~(-6) M～5×10~(-5)M)对培养心肌细胞搏动强度(dv/dt)有明显抑制作用,而对搏动频率无明显影响。噻吗心安也可明显抑制异丙肾上腺素增加dv/dt及搏动频率的作用;拮抗异丙肾上腺素(5×10~(-5)M)增加cAMP含量及腺苷环化酶活性的作用。本文还观察到噻吗心安对培养心肌细胞的缺氧缺糖性损伤具保护作用。上述结果在细胞分子水平上进一步证明了噻吗心安通过阻断β受体而发挥其药理作用。
In this study, timolol (5×10-6 M～5×10-5 M) was observed to have a significant inhibitory effect on the beat intensity (dv/dt) of cultured myocardial cells, but had no significant effect on beat frequency. Timolol also significantly inhibited the effect of isoproterenol on increasing dv/dt and beating frequency, and antagonized the effect of isoproterenol (5×10 -5 M) on cAMP content and adenylyl cyclase activity. This article also observed that timolol has a protective effect on oxygen-glucose deprivation in cultured cardiomyocytes. The above results further demonstrate that timolol exerts its pharmacological effects by blocking beta receptors at the cellular and molecular level.