Selectivity of dihydropyridines for cardiac L-type and sympathetic N-type Ca2+ channels.
Selectivity of dihydropyridines for cardiac L-type and sympathetic N-type Ca2+ channels.
复制标题
二氢吡啶对心脏 L 型和交感神经 N 型 Ca2 通道的选择性。
DOI：
10.1016/s0014-2999(99)00237-x
复制
发表时间：
1999
影响因子：
5
通讯作者：
Norio Akaike
中科院分区：
文献类型：
--
作者：
H. Uneyama;H. Uchida;T. Konda;Ryota Yoshimoto;Norio Akaike
用全细胞膜片钳技术研究了西尼地平和其他二氢吡啶类药物对心肌L型钙通道（伊卡，L）和交感神经N型钙通道电流（伊卡，N）的阻断作用。在-80 mV时，西尼地平在低于1 μM的浓度下对伊卡，L几乎没有抑制作用（IC 50值; 17 μM）。1 μM西尼地平使伊卡，L的稳态失活曲线向负电位方向移动，但不改变电流-电压关系。西尼地平的每个动作的特征在于优先于静息通道的失活通道的高亲和力。二氢吡啶类化合物对伊卡，L的IC_（50）值在0.01 ~ 10 μM之间，对伊卡，N的IC_（50）值在3 ~ 30 μM之间。西尼地平对伊卡、N的亲和力最强。这些结果表明，西尼地平并没有通过抑制心脏L-型通道，但通过交感神经N-型通道阻滞引起的心动过速缺陷。
The blocking effects of cilnidipine and other dihydropyridines on L-type cardiac Ca2+channels (ICa,L) and N-type sympathetic Ca2+channel currents (ICa,N) were studied using a whole-cell patch-clamp technique. At −80 mV, cilnidipine had little inhibitory effect below concentrations of 1 μM on ICa,L(IC50value; 17 μM). However, 1 μM cilnidipine strongly shifted the steady-state inactivation curve of ICa,Ltoward negative potentials without changing the current–voltage relationship. Each action of cilnidipine was characterized by a high affinity for the inactivated channel in preference to the resting channel. The IC50values of dihydropyridines for ICa,Lwere in the range between 0.01 and 10 μM, and those for ICa,Nwere between 3 and 30 μM. Cilnidipine had the strongest affinity for ICa,Namong the dihydropyridines tested. These results suggest that cilnidipine did not cause hypotension-evoked tachycardia deficiency by depression of cardiac L-type channels but by sympathetic N-type channels blockade.
钙进入阻断对左心室收缩和舒张功能的影响。
影响因子：
37.8
作者：
Walsh,RA
通讯作者：
Walsh,RA