Honma M, Ui M
Eur J Pharmacol. 1978 Jan 1;47(1):1-10. doi: 10.1016/0014-2999(78)90367-9.
S.c. injections of cholinergic agents, carbachol, methacholine and bethanechol, into fasted rats caused rapid increases in the plasma concentration of cyclic GMP, with a sharp peak at 5--10 min after the injection. Acetylcholine gave rise to a rapid accumulation of cyclic GMP in plasma only when administered together with physostigmine which produced only a slight, if any, potentiation of the action of the cholinesterase-resistant choline esters. Cyclic AMP also increased after these drugs, but only subsequently to the rise of cyclic GMP; the primary action of the cholinergic drugs appeared to be the increase in cyclic GMP. Atropine was effective not only in abolishing the increase in plasma cyclic GMP induced by cholinergic drugs but also in lowering the baseline level of cyclic GMP. It was concluded that the plasma concentration of cyclic GMP could serve as a good parameter of cholinergic activity in rats.
给禁食的大鼠皮下注射胆碱能药物、卡巴胆碱、乙酰甲胆碱和氨甲酰甲胆碱后,血浆环鸟苷酸(cGMP)浓度迅速升高,注射后5 - 10分钟出现一个尖峰。只有当乙酰胆碱与毒扁豆碱一起给药时,才会导致血浆中cGMP迅速积累,而毒扁豆碱对这些抗胆碱酯酶胆碱酯类药物的作用即使有增强,也很轻微。这些药物注射后环磷酸腺苷(cAMP)也会增加,但仅在cGMP升高之后;胆碱能药物的主要作用似乎是增加cGMP。阿托品不仅能消除胆碱能药物引起的血浆cGMP升高,还能降低cGMP的基线水平。得出的结论是,血浆cGMP浓度可作为大鼠胆碱能活性的一个良好参数。