| 丁苄腈心安与心得安对大鼠心肌β肾上腺素受体亲和力比较 |
| |
| 引用本文： | 戴德哉,戴岳,王路阳,黄枕亚. 丁苄腈心安与心得安对大鼠心肌β肾上腺素受体亲和力比较[J]. 中国药理学通报, 1987, 0(6) |
| |
| 作者姓名： | 戴德哉 戴岳 王路阳 黄枕亚 |
| |
| 作者单位： | 中国药科大学药理研究室 南京(戴德哉，戴岳，王路阳)，中国药科大学药理研究室 南京(黄枕亚) |
| |
| 基金项目： | 江苏省卫生厅科研基金资助 |
| |
| 摘 要： | 本文以~3H双氢心得舒(~3H—DHA)作为放射性配基,测定大鼠心肌上β肾上腺素受体的最大结合容量(B_(max))和平衡解离常数(K_D)分别为104.1±4.7fmol/mg蛋白质及10.1±2.7nM,Hill系数(nH)为1.007±0.002。丁苄腈心安和心得安对大白鼠心肌β肾上腺素能受体与~3H-DHA结合的半数抑制浓度(IC_(50))分别为3.30±0.74×10~(-8)M和3.87±0.66×10~(-7)M,表观解离常数各为2.20±0.49×10~(-8)及2.58±0.44×10~(-7)。故丁苄腈心得安对大鼠心肌β肾上腺素受体的亲和力约为心得安的11.7倍。
|
| 关 键 词： | β肾上腺素受体 ~3H-DHA 丁苄腈心安 心得安 |
THE COMPARSION OF AFFINITY BETWEEN BUNITROLOL AND PROPRANOLOL TO MYOCARDIAL B-ADRENERGIC RECE- PTORS |
| |
| Dai Dezai,Dai Yue,Wang Luyang,et al. THE COMPARSION OF AFFINITY BETWEEN BUNITROLOL AND PROPRANOLOL TO MYOCARDIAL B-ADRENERGIC RECE- PTORS[J]. Chinese Pharmacological Bulletin, 1987, 0(6) |
| |
| Authors: | Dai Dezai Dai Yue Wang Luyang et al |
| |
| Abstract: | The maximum specific binding(Bmax)and the dissociation constants(K D) of 8H -dihydroalprenolol in rat myocardial membrane are 104.1 +4. 7 fmol/mg protein and 10.1+2.7nM, respectively, and the Hill coeffici-ent(nn) is equal to 1.007+0.002. The half inhibition concentration concentration ( IC50) of bunitrolol and propranolol on 3H - dihydroal- prcnolol binding to myocardial B-adrenergic receptors are 3.30+ 0. 74 x 10- 8M ,and 3. 87+0.66 x 10-7M , the apparant dissociation constants (Kl) are 2.2+0.48x10-8M and 2.58+0.44x10-7M, respectively. The affinity of bunitrolol to myocardial B-adrener-gic receptors is 11.7 times as potent as propra'nolol. |
| |
| Keywords: | B-adrenefgic receptor 3H-dihydroalprenoiol bunit- rolol proprauolol |
| 本文献已被 CNKI 等数据库收录！ |
