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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >The dihydropyridine analogue cerebrocrast blocks both T-type and L-type calcium currents.
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The dihydropyridine analogue cerebrocrast blocks both T-type and L-type calcium currents.

机译：二氢吡啶类似物的脑裂剂可阻断T型和L型钙电流。

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摘要

Cerebrocrast is a novel lipophilic dihydropyridine derivative with potential neuroprotective and antidiabetic properties. We have analyzed its interaction with L-type (CaV1.2b) and T-type (CaV3.1) calcium channels using a whole-cell patch clamp in HEK 293 cells. Cerebrocrast inhibited current flux through both CaV1.2b and CaV3.1 channels. In both cases, the drug was about 10-fold less effective than neutral dihydropyridines, but more efficient than the charged dihydropyridine amlodipine. IC50 values for the CaV1.2b channel were 586 +/- 96 nmol/L and 178 +/- 78 nmol/L at holding potentials of -80 mV and -50 mV, respectively. Approximately 50 micromol/L of cerebrocrast was needed to block 50% of the current amplitude in the CaV3.1 channel, but this inhibition was not facilitated by shifting the holding potential from -100 mV to -70 mV. Cerebrocrast did not alter current kinetics in either investigated channel, and the inhibition of calcium current was partly reversible or irreversible. In conclusion, the interaction of cerebrocrast with CaV3.1 lacked the typical characteristics of a state-dependent interaction, and voltage-dependent inhibition of CaV1.2b was consistent with partial interaction with the inactivated state of the channel.
机译：脑cra是一种新型的亲脂性二氢吡啶衍生物，具有潜在的神经保护和抗糖尿病特性。我们已经使用HEK 293细胞中的全细胞膜片钳分析了其与L型（CaV1.2b）和T型（CaV3.1）钙通道的相互作用。脑颅抑制了通过CaV1.2b和CaV3.1通道的电流通量。在这两种情况下，该药物的效力均比中性二氢吡啶低约10倍，但比带电荷的二氢吡啶氨氯地平更有效。在保持电势为-80 mV和-50 mV时，CaV1.2b通道的IC50值分别为586 +/- 96 nmol / L和178 +/- 78 nmol / L。需要大约50 micromol / L的脑脊液来阻断CaV3.1通道中50％的电流振幅，但是通过将保持电位从-100 mV转移到-70 mV并不能促进这种抑制。在任何一个被研究的通道中脑脊液都没有改变电流动力学，并且对钙电流的抑制是部分可逆的或不可逆的。总之，脑脊液与CaV3.1的相互作用缺乏状态依赖性相互作用的典型特征，并且CaV1.2b的电压依赖性抑制作用与通道失活状态的部分相互作用相一致。

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