Janis R A, Shrikhande A V, Johnson D E, McCarthy R T, Howard A D, Greguski R, Scriabine A
Institute for Preclinical Pharmacology, Miles Inc., West Haven, CT 06516.
FEBS Lett. 1988 Nov 7;239(2):233-6. doi: 10.1016/0014-5793(88)80923-2.
Bovine brain was subjected to acid extraction and several purification steps. A fraction from brain that eluted from C18 reverse-phase columns at 30-35% acetonitrile inhibited [3H]nitrendipine binding to cardiac membranes. Further purification of this fraction on a sizing column in the presence of 40% acetonitrile yielded a low molecular mass fraction (less than 1 kDa) that produced a time- and voltage-dependent inhibition of L-type (but not T-type) Ca2+-channel current in GH3 cells. The results suggest that this fraction contains an endogenous substance that binds directly to slowly-inactivating Ca2+ channels and thereby inhibits current flow.
牛脑经过酸提取和多个纯化步骤。从C18反相柱上以30 - 35%乙腈洗脱的脑部分馏物可抑制[3H]尼群地平与心肌膜的结合。在40%乙腈存在下，将该部分馏物在尺寸排阻柱上进一步纯化，得到一个低分子量部分馏物（小于1 kDa），该部分馏物对GH3细胞中的L型（而非T型）Ca2 +通道电流产生时间和电压依赖性抑制。结果表明，该部分馏物含有一种内源性物质，它直接与缓慢失活的Ca2 +通道结合，从而抑制电流流动。
