Lucchelli A, Boselli C, Grana E
Istituto di Farmacologia, Università di Pavia, Italy.
Farmaco Sci. 1987 Sep;42(9):619-27.
Dissociation constant and relative efficacy values of six cholinergic agents endowed with a high muscarinic activity (carbachol, methylfurtrethonium, cis-2-methyl-4-trimetylammoniummethyl-1,3-dioxolane, cis-2-methyl-5-trimethylammoniummethyl-1,3-oxathiolane, muscarone, oxotremorine) have been determined on the frog rectus abdominis nicotinic receptors. The results obtained point out that: a) the nicotinic receptor reserve of the frog rectus abdominis is very little if any, b) there are no appreciable variations in the relative efficacy values of all the compounds tested, c) it is instead possible to establish a rank order of affinity. The comparison of the affinity values towards nicotinic receptors, herewith reported, and those towards ileal muscarinic receptors, previously reported could be useful to shed some light on the differences between muscarinic and nicotinic receptors.
已在青蛙腹直肌烟碱样受体上测定了六种具有高毒蕈碱活性的胆碱能药物（卡巴胆碱、甲基呋罗溴铵、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、毒蝇蕈酮、氧化震颤素）的解离常数和相对效价。所得结果表明：a）青蛙腹直肌的烟碱样受体储备极少（如果有的话）；b）所有受试化合物的相对效价值没有明显变化；c）相反，可以确定亲和力的等级顺序。本文报道的对烟碱样受体的亲和力值与先前报道的对回肠毒蕈碱样受体的亲和力值进行比较，可能有助于阐明毒蕈碱样受体和烟碱样受体之间的差异。
