Barlow R B
J Pharm Pharmacol. 1978 Nov;30(11):703-10. doi: 10.1111/j.2042-7158.1978.tb13369.x.
The effects of a hydroxyl group on the activity and affinity of compounds related to n-pentyltrimethylammonoum have been studied on the guinea-pig ileum, frog rectus, acetylcholinesterase and on partitioning (Rm) and size (phiov, Vm). The hydroxyl group lowered affinity in all tests, confirming the importance of hydrophobic forces in binding to receptors. Activity on the ileum was lowered appreciably but on the rectus only slightly. The effects on Rm did not indicate any interactions between hydroxyl, onium group and water but the apparent size of the hydroxyl group (deltaphiov) depends on the nature of the onium group.
已在豚鼠回肠、蛙腹直肌、乙酰胆碱酯酶以及分配系数(Rm)和分子大小(φov、Vm)方面研究了羟基对与正戊基三甲基铵相关化合物的活性和亲和力的影响。在所有测试中,羟基均降低了亲和力,这证实了疏水作用力在与受体结合中的重要性。对回肠的活性有明显降低,但对腹直肌的活性仅略有降低。对Rm的影响未表明羟基、鎓离子基团与水之间存在任何相互作用,但羟基的表观大小(δφov)取决于鎓离子基团的性质。