Wojcikiewicz R J, Dobson P R, Brown B L
Biochim Biophys Acta. 1984 Sep 14;805(1):25-9. doi: 10.1016/0167-4889(84)90032-6.
Acetylcholine, oxotremorine and carbachol, compounds that exhibit muscarinic agonist activity, maximally inhibited basal prolactin secretion from GH3 cells by approx. 50% and intracellular cyclic AMP levels by approx. 20%. Both parameters were inhibited with similar potencies by each agonist. These inhibitory effects were blocked by a muscarinic but not by a nicotinic receptor antagonist. In the presence of VIP or IBMX, which raise intracellular cyclic AMP levels and stimulate hormone release, the degree of muscarinic inhibition was increased, but the potency remained unchanged. Similar changes in the secretory rate of prolactin and growth hormone occurred in these and in cell perifusion experiments. These results suggest that the inhibition of hormone secretion from GH3 cells by muscarinic agonists is mediated by a decrease in intracellular cyclic AMP levels.
乙酰胆碱、氧化震颤素和卡巴胆碱这些具有毒蕈碱激动剂活性的化合物,可使GH3细胞的基础催乳素分泌最大程度地受到约50%的抑制,细胞内环状AMP水平受到约20%的抑制。每种激动剂对这两个参数的抑制效力相似。这些抑制作用可被毒蕈碱受体拮抗剂阻断,而不能被烟碱受体拮抗剂阻断。在存在能提高细胞内环状AMP水平并刺激激素释放的血管活性肠肽(VIP)或异丁基甲基黄嘌呤(IBMX)的情况下,毒蕈碱抑制的程度增加,但效力保持不变。在这些实验以及细胞灌流实验中,催乳素和生长激素的分泌速率也出现了类似变化。这些结果表明,毒蕈碱激动剂对GH3细胞激素分泌的抑制作用是由细胞内环状AMP水平的降低介导的。