他克林可阻断海马神经元中的电压依赖性离子通道。
Tetrahydroaminoacridine blocks voltage-dependent ion channels in hippocampal neurons.
作者信息
Rogawski M A
机构信息
Medical Neurology Branch, National Institute of Neurological and Communicative Disorders and Stroke, Bethesda, MD 20892.
出版信息
Eur J Pharmacol. 1987 Oct 6;142(1):169-72. doi: 10.1016/0014-2999(87)90670-4.
Tetrahydroaminoacridine (THA) is a centrally active anticholinesterase that may produce functional improvement in patients with Alzheimer's disease. Because of its structural similarity to the potassium channel (A-current) blocking drug 4-aminopyridine (4-AP), it has been speculated that some of the therapeutic benefit of THA might result from inhibition of potassium currents. In the present study, THA produced a dose-dependent, reversible block of the A-current in cultured hippocampal neurons (IC50, 30 microM). However, at similar concentrations it also inhibited other voltage-dependent currents.
四氢氨基吖啶（THA）是一种中枢活性抗胆碱酯酶药物，可能会使阿尔茨海默病患者的功能得到改善。由于其结构与钾通道（A电流）阻断药物4-氨基吡啶（4-AP）相似，有人推测THA的一些治疗益处可能源于对钾电流的抑制。在本研究中，THA在培养的海马神经元中产生了剂量依赖性、可逆性的A电流阻断（IC50为30 microM）。然而，在相似浓度下，它也抑制其他电压依赖性电流。
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