Barlow R B, Ramtoola S
Br J Pharmacol. 1980;71(1):31-4. doi: 10.1111/j.1476-5381.1980.tb10905.x.
1 From measurements of the affinity constants of hydratropyltropine and its methiodide for muscarine-sensitive acetylcholine receptors in the guinea-pig ileum, the increment in log K for the hydroxyl group in atropine is 2.06 and in the methiodide it is 2.16. These effects are slightly bigger than any so far recorded with these receptors. 2 The estimate of the increment in apparent molal volume for the hydroxyl group is 1.1 cm3/mol in atropine and 1.0 cm3/mol in the methobromide. 3 The large effect of the group on affinity may be linked to its small apparent size in water as suggested in the previous paper.
1 根据对水合莨菪碱及其甲碘化物与豚鼠回肠中对毒蕈碱敏感的乙酰胆碱受体的亲和常数的测量，阿托品中羟基的log K增量为2.06，甲碘化物中为2.16。这些效应比迄今为止用这些受体记录到的任何效应都略大。2 阿托品中羟基的表观摩尔体积增量估计为1.1 cm³/mol，甲溴化物中为1.0 cm³/mol。3 如前一篇论文所述，该基团对亲和力的巨大影响可能与其在水中较小的表观尺寸有关。
