Järv J, Toomela T, Karelson E
Institute of Chemical Physics, University of Tartu, Estonia.
Biochem Mol Biol Int. 1993 Jul;30(4):649-54.
The carbachol-mediated inhibition of cAMP synthesis in membranes of rat cerebral cortex revealed maximum in 0.3 mM carbachol solution, while further increases of the drug concentration blocked the inhibitory effect and restored the adenylate cyclase activity. The bell-shaped dose-response curve was analyzed assuming that carbachol binds with two distinct sites on muscarinic receptor, which are responsible for agonistic and antagonistic effects, related to this receptor. The pKagon and pKant values for carbachol were 5.0 and 2.1, respectively.
卡巴胆碱介导的大鼠大脑皮质膜中cAMP合成的抑制作用在0.3 mM卡巴胆碱溶液中达到最大值，而药物浓度的进一步增加则阻断了抑制作用并恢复了腺苷酸环化酶活性。假设卡巴胆碱与毒蕈碱受体上两个不同的位点结合，这两个位点分别负责与该受体相关的激动和拮抗作用，对钟形剂量反应曲线进行了分析。卡巴胆碱的pKagon和pKant值分别为5.0和2.1。
