Drug mechanism of action

Lozenges for the treatment of sore throat provide relief of discomfort in cases of oral inflammation.

药物作用机制

口腔发炎时服用润喉糖可以缓解咽喉肿痛所带来的不适。

This effect has not been fully explained so far.

到目前为止，润喉糖的这一效用还没有得到充分的解释。

Here, we have examined the proposition that key components of pharmaceutical preparations for the treatment of sore throat which are routinely regarded antiseptics might have sodium channel- blocking, i.e. local anaesthetic-like effects.

用于治疗咽喉肿痛的药物制剂的主要成分通常被认为是抗菌剂，在此，我们研究了这些药物成分可能具有钠离子通道阻滞作用——即局部麻醉样作用——这一命题。

We investigated the effects of hexylresorcinol, amylmetacresol and dichloro- benzylalcoholonvoltage-operatedneuronal(NaV1.2) sodium channels heterologously expressed in HEK 293 cells in vitro.

我们研究了间苯二酚、戊间甲酚和二氯苄醇对表达在 HEK293 细胞上的异源性电压门控神经元钠离子通道（NaV1.2）的影响。

Hexylresorcinol, amylmetacresol and dichloro-benzylalcohol reversibly blocked depolarisation-induced whole-cell sodium inward currents.

间苯二酚、戊间甲酚和二氯苄醇可逆性地阻断了去极化引起的全细胞钠离子内向电流。

The half-maximum blocking concentrations (EC50) at−150 mV were 23.1, 53.6 and 661.6 µM, respectively.

- 150 毫伏时的半数阻滞浓度（EC50）分别为 23.1、53.6 和 661.6 微摩尔。

Block induced by hexylresorcinol and amylme- tacresol was increased at depolarised potentials and use-dependent during trains of depolarisations applied at high frequency (100 Hz) indicating that both drugs bind more tightly to inactivated conformations of the channel.

间苯二酚和戊间甲酚所致的阻滞在去极化电位时升高且在施加高频率（100赫兹）去极化脉冲系列时呈现出使用依赖性，这一结果表明两种药物与钠离子通道的灭活构象的结合更紧密。

Estimates for the inactivated state affinity were 1.88 and 35 µM for hexylresorcinol and amylmetacresol, respectively.

间苯二酚和戊间甲酚与灭活构象的结合亲和力的估计值分别为 1.88 和 35 微摩尔