豚鼠心房起搏细胞在29℃时以及回肠在29℃和37℃时毒蕈碱敏感性乙酰胆碱受体亲和常数的比较。
A comparison of affinity constants for muscarine-sensitive acetylcholine receptors in guinea-pig atrial pacemaker cells at 29 degrees C and in ileum at 29 degrees C and 37 degrees C.
作者信息
Barlow R B, Berry K J, Glenton P A, Nilolaou N M, Soh K S
出版信息
Br J Pharmacol. 1976 Dec;58(4):613-20. doi: 10.1111/j.1476-5381.1976.tb08631.x.
Abstract
1 The affinity of 17 compounds for muscarine-sensitive acetylcholine receptors in atrial pacemaker cells and ileum of the guinea-pig has been measured at 29 degrees C in Ringer-Locke solution. Measurements were also made at 37 degrees C with 7 of them. 2 Some of the compounds had much higher affinity for the receptors in the ileum than for those in the atria. For the most selective compound, 4-diphenylacetoxy-N-methylpiperidine methiodide, the difference was approximately 20-fold. The receptors in the atria are therefore different the structure from those in the ileum. 3 The effect of temperature on affinity are not the same for all the compounds, tested indicating different enthalpies and entropies of adsorption and accounting for some of the difficulty experienced in predicting the affinity of new compounds.
摘要
在29摄氏度的林格-洛克溶液中，测定了17种化合物对豚鼠心房起搏细胞和回肠中对毒蕈碱敏感的乙酰胆碱受体的亲和力。还对其中7种化合物在37摄氏度下进行了测定。
一些化合物对回肠中的受体的亲和力比对心房中的受体的亲和力高得多。对于最具选择性的化合物4-二苯基乙酰氧基-N-甲基哌啶甲碘化物，差异约为20倍。因此，心房中的受体与回肠中的受体结构不同。
温度对亲和力的影响并非对所有测试化合物都相同，这表明吸附的焓和熵不同，也解释了预测新化合物亲和力时遇到的一些困难。
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