Nifedipine, diltiazem, bepridil and verapamil uptakes into cardiac and smooth muscles.
Nifedipine, diltiazem, bepridil and verapamil uptakes into cardiac and smooth muscles.
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硝苯地平、地尔硫卓、苯普地尔和维拉帕米被心脏和平滑肌吸收。
DOI：
10.1016/0014-2999(83)90330-8
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发表时间：
1983
影响因子：
5
通讯作者：
Sperelakis,N
中科院分区：
文献类型：
--
作者：
Pang,DC;Sperelakis,N
Vogel等人，(1979; J Pharmacol. Exp. Ther. 210，378）报道了一种钙拮抗剂苄普地尔（bepridil）在内部发挥作用以及其对阻断心肌中的Ca 2+进入的作用。因此，氚硝苯地平，地尔硫卓，苄普地尔，维拉帕米的猫回肠平滑肌，鸡胚心室肌，和兔乳头肌的摄取进行了研究。结果表明，维拉帕米和苄普地尔的肌肉摄取量远高于硝苯地平和地尔硫卓。苄普地尔的摄取明显大于维拉帕米;因此，摄取顺序为：苄普地尔>维拉帕米>硝苯地平>地尔硫卓。心肌积累的钙拮抗剂的量至少是平滑肌的2倍。由肌肉积累的给定钙拮抗剂的量不是该钙拮抗剂抑制Ca 2+摄取到肌肉中的能力的函数，因为硝苯地平和地尔硫卓在抑制Ca 2+摄取方面更有效，但具有最小的摄取。钙拮抗剂对平滑肌钙摄取的抑制作用强于心肌。计算表明，心脏和平滑肌稳态时的内部药物浓度等于（地尔硫卓）或远高于介质中的药物浓度（苄普地尔和维拉帕米）。可以得出结论，苄普地尔和维拉帕米进入和积累在肌肉细胞，而硝苯地平和地尔硫卓渗透到肌肉中更缓慢。所有四种药物进入肌肉细胞的能力赋予了这些钙拮抗剂可能对肌肉的内部部位（如肌浆网）发挥次级作用的可能性。
Vogel et al., (1979; J Pharmacol. Exp. Ther. 210, 378) reported that one calcium antagonist, bepridil, exerted an effect internally as well as its effect on blocking Ca2+entry in cardiac muscle. Therefore, the uptakes of tritiated nifedipine, diltiazem, bepridil, and verapamil by cat ileal smooth muscle, chick embryonic ventricular muscle, and rabbit papillary muscle were investigated. It was found that the uptakes of verapamil and bepridil by the muscle were much higher than those of nifedipine and diltiazem. The uptake of bepridil was substantially greater than that of verapamil; thus, the order of uptake was: bepridil > verapamil > > nifedipine > diltiazem. The cardiac muscles accumulated at least 2-fold greater amount of calcium antagonists that the smooth muscle. The amount of a given calcium antagonist accumulated by a muscle was not a function of the ability of that calcium antagonist to inhibit Ca2+uptake into the muscle, since nifedipine and diltiazem were more potent in depressing Ca2+uptake, but had the smallest uptakes. The calcium antagonists were more effective in depressing Ca2+uptake into smooth muscle than into cardiac muscle. Calculation indicates that internal drug concentration at steady state for both cardiac and smooth muscles was either equal to (diltiazem) or much higher than the drug concentration in the medium (bepridil and verapamil). It is concluded that bepridil and verapamil enter and accumulate in the muscle cells, whereas nifedipine and diltiazem permeate more slowly into muscles. The ability of all four drugs to enter the muscle cells confers the possibility that these calcium antagonists may exert secondary actions on internal sites of the muscle, such as the sarcoplasmic reticulum.
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快速分离分离的大鼠肝细胞的颗粒成分和可溶性细胞质。
DOI：
10.1016/0005-2728(74)90022-x
发表时间：
1974
期刊：
Biochimica et biophysica acta
影响因子：
--
作者：
P. Zuurendonk;J. Tager
通讯作者：
J. Tager
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DOI：
10.1159/000158206
发表时间：
1979
期刊：
Blood vessels
影响因子：
--
作者：
D. Harder;N. Sperelakis
通讯作者：
N. Sperelakis
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影响因子：
3
作者：
S. Mras;N. Sperelakis
通讯作者：
N. Sperelakis
地尔硫卓对豚鼠离体心室肌电和机械活动的影响。
DOI：
--
发表时间：
1975
期刊：
Japanese Journal of Pharmacology
影响因子：
--
作者：
H. Nakajima;M. Hoshiyama;K. Yamashita;A. Kiyomoto
通讯作者：
A. Kiyomoto
生物活性1,4-二氢吡啶衍生物
影响因子：
0.2
作者：
J. Prous;P. Blancafort;J. Castaǹer;M. Serradell;N. Mealy
通讯作者：
N. Mealy