首页> 美国卫生研究院文献>British Journal of Pharmacology and Chemotherapy >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.
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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.

机译:在29摄氏度的豚鼠心房起搏器细胞和29摄氏度和37摄氏度的回肠中对毒蕈碱敏感的乙酰胆碱受体的亲和常数的比较。

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摘要

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.
机译:1在林格-洛克溶液中,在29摄氏度下测量了17种化合物对心房起搏器细胞和豚鼠回肠中毒蕈碱敏感的乙酰胆碱受体的亲和力。还在37摄氏度下进行了7次测量。 2有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。对于选择性最高的化合物4-二苯基乙酰氧基-N-甲基哌啶甲硫醇,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。 3温度对所有化合物的亲和力影响都不相同,经测试表明吸附的焓和熵不同,并解释了预测新化合物亲和力时遇到的一些困难。

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