Khromov-Borisov N V, Danilov A F, Indenbom M L, Tikhonova L N, Lavrent'eva V V
Farmakol Toksikol. 1975 Nov-Dec;38(6):683-7.
The intrinsic alpha activities and the D2 (frog, m, rectus abdominalis) concentrations were estimated for different acetylcholine and sebacinylcholine derivatives. So were also the A2 values for antagonists and the affinity constants Kc for some partial agonists. The results obtained disprove Paton's "rate-theory". The relationship between the cholinergic activity and the volume of cationic groups was studied and it could not possibly be explained by the steric hindrance alone. It is suggested that certain hydrophobic radicals of the cationic groups contact the receptor surface outside the anionic centre. Such contacts prevent the cholinoreceptor to change its conformation and thus inhibit the depolarization of the membrane. An approximate estimation of the anionic site dimensions is given.
针对不同的乙酰胆碱和癸二酰胆碱衍生物，测定了其固有α活性和D2（青蛙，肌肉，腹直肌）浓度。同时也测定了拮抗剂的A2值和一些部分激动剂的亲和常数Kc。所得结果反驳了帕顿的“速率理论”。研究了胆碱能活性与阳离子基团体积之间的关系，仅靠空间位阻无法解释这种关系。有人提出，阳离子基团的某些疏水基团在阴离子中心之外与受体表面接触。这种接触会阻止胆碱能受体改变其构象，从而抑制膜的去极化。给出了阴离子位点尺寸的近似估计值。
