Adams P R
Pflugers Arch. 1975 Oct 28;360(2):145-53. doi: 10.1007/BF00580537.
The agonist concentration--endplate conductance relation was examined for a number of agonists (such as carbachol, alkyl trimethylammonium salts, choline and decamethonium). The endplate current evoked varied as Imax [a/(a + K)]2, where a is the agonist concentration and Imax and K are agonist-specific parameters. This finding suggests that the endplate receptor has 2 equivalent subunits which bind agonist approximately non-cooperatively. The liganded subunits then switch to an active conformation with a probability that depends on the nature of the agonist. Both subunits must adopt the active conformation for the channel to open, but the transitions of the subunits could be either independent or concerted.
研究了多种激动剂(如卡巴胆碱、烷基三甲基铵盐、胆碱和十烃季铵)的激动剂浓度与终板电导的关系。诱发的终板电流变化符合Imax [a/(a + K)]2,其中a为激动剂浓度,Imax和K是激动剂特异性参数。这一发现表明,终板受体有2个等效亚基,它们以近似非协同的方式结合激动剂。然后,结合了配体的亚基以取决于激动剂性质的概率转变为活性构象。两个亚基都必须采用活性构象通道才能打开,但亚基的转变可以是独立的,也可以是协同的。