Lucchelli A, Boselli C, Grana E
Farmaco Sci. 1986 Mar;41(3):175-82.
The nicotinic activity of seven cholinergic agents endowed with a very high muscarinic activity (carbachol, methylfurtrethonium, cis-2-methyl-4-trimethylammoniummethyl-1,3-dioxolane, cis-2-methyl-5-trimethylammoniummethil-1,3-oxathiolane, muscarine, muscarone, oxotremorine) has been studied on the frog rectus abdominis. Carbachol is the most active compound with an EC50 value of 1.98 X 10(-6) M; the ratio between nicotinic and muscarinc activity is 67. Methylfurtrethonium and oxotremorine are the least potent and also behave as "partial agonists". Muscarine is devoid of activity. It is concluded that the nicotinic component does not interfere with the evaluation of the muscarinic potency of the compounds under investigation.
在青蛙腹直肌上研究了七种具有非常高毒蕈碱活性的胆碱能药物（卡巴胆碱、甲基呋索氯铵、顺式-2-甲基-4-三甲基铵甲基-1,3-二氧戊环、顺式-2-甲基-5-三甲基铵甲基-1,3-氧硫杂环戊烷、毒蕈碱、毒蕈酮、氧化震颤素）的烟碱活性。卡巴胆碱是最具活性的化合物，EC50值为1.98×10(-6)M；烟碱活性与毒蕈碱活性之比为67。甲基呋索氯铵和氧化震颤素效力最低，且表现为“部分激动剂”。毒蕈碱无活性。结论是，烟碱成分不干扰所研究化合物毒蕈碱效力的评估。
