离子强度对心肌毒蕈碱受体的影响。
The effect of ionic strength on cardiac muscarinic receptors.
作者信息
Burgen A S
出版信息
Br J Pharmacol. 1986 Jun;88(2):451-5. doi: 10.1111/j.1476-5381.1986.tb10223.x.
Abstract
The binding of N-methylscopolamine (NMS) and carbachol to muscarinic receptors in the rat heart has been measured as a function of ionic strength (mu). The binding of NMS was reduced by 3.69 fold for a 10 fold increase in ionic strength. The binding of carbachol was affected in two ways. Firstly, the proportions of the subsites were changed. Above mu = 0.5 M, the superhigh (SH) subsite was converted into the low (L) subsite and above mu = 0.8 M, the high (H) subsite was also converted into the L subsite. Therefore, at high ionic strength, no agonist-determined subsites can be detected. In addition, increase in ionic strength reduced the binding of carbachol to all subsites and to a much greater extent than for NMS.
摘要
已测定了N-甲基东莨菪碱（NMS）和卡巴胆碱与大鼠心脏毒蕈碱受体的结合情况，并将其作为离子强度（μ）的函数。离子强度每增加10倍，NMS的结合减少3.69倍。卡巴胆碱的结合受到两方面影响。首先，亚位点的比例发生了变化。在μ＞0.5M时，超高（SH）亚位点转变为低（L）亚位点，在μ＞0.8M时，高（H）亚位点也转变为L亚位点。因此，在高离子强度下，无法检测到激动剂决定的亚位点。此外，离子强度增加降低了卡巴胆碱与所有亚位点的结合，且降低程度比NMS大得多。
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