Vislobokov A I, Marysheva V V, Shabanov P D
St. Petersburg State Military Medical Academy, Ministry of Defense of the Russian Federation, ul. Lebedeva 6, St. Petersburg, 194044 Russia.
Eksp Klin Farmakol. 2003 Nov-Dec;66(6):9-11.
Membranotropic effects of the antihypoxants bemithyl and almide, structural analogs of thiobenzimidazole, have been studied on the isolated neuronal preparations of Lymaea stagnalis branchycephalic mollusk. Both drugs in a concentration range of 100-1000 microM produced a reversible, dose-dependent nonselective single-phase blocking action upon the ion channels and completely blocked the channels at a concentration of 10 mM. Therefore, bemithyl and almide are active membranotropic compounds capable (in sufficiently high concentrations) of changing the conductivity of slow sodium, calcium, and potassium ion channels in excitable cells. The protective antihypoxant drug reactions on a systemic level of the organism are probably related to the fact that both drugs in small concentrations are capable of hyperpolarizing the cell membrane, activating the ion channel function, and stabilizing the action potential under hypoxia conditions; in greater concentrations, bemithyl and almide are capable of blocking ion currents, thus reducing the excitability of cells and protecting them from overstress.
已在隔离的椎实螺（Lymaea stagnalis）短头软体动物神经元制剂上研究了抗缺氧剂贝米噻（bemithyl）和阿尔米德（almide）（硫代苯并咪唑的结构类似物）的亲膜效应。两种药物在100 - 1000微摩尔浓度范围内对离子通道产生可逆的、剂量依赖性的非选择性单相阻断作用，并在10毫摩尔浓度时完全阻断通道。因此，贝米噻和阿尔米德是活性亲膜化合物，能够（在足够高的浓度下）改变可兴奋细胞中慢钠、钙和钾离子通道的电导率。该保护性抗缺氧药物在机体系统水平上的反应可能与以下事实有关：两种药物在低浓度时能够使细胞膜超极化，激活离子通道功能，并在缺氧条件下稳定动作电位；在较高浓度时，贝米噻和阿尔米德能够阻断离子电流，从而降低细胞兴奋性并保护它们免受过度应激。
