Raffa R B, Ortegón M E, Watson M
Department of Biological Research, Janssen Research Foundation, Spring House, PA 19477.
Eur J Pharmacol. 1988 Dec 13;158(3):289-92. doi: 10.1016/0014-2999(88)90082-9.
We have previously proposed that the reciprocal hindlimb scratching (RHS) of mice elicited by intrathecal injection of muscarinic agents is mediated by M1 muscarinic receptors. In this study, benzhexol potently inhibited pilocarpine-induced RHS (ID50 = 0.5 ng), methoctramine did not fully block RHS and RS 86 neither produced nor blocked RHS. These data (1) differentiate the three muscarinic agents using this in vivo endpoint, (2) substantiate binding studies characterizing benzhexol and methoctramine as putative M2 and M2 antagonists, respectively, and (3) further support using RHS for studying muscarinic agents.
我们之前曾提出,鞘内注射毒蕈碱剂引发的小鼠后肢交互搔抓(RHS)是由M1毒蕈碱受体介导的。在本研究中,苯海索能有效抑制毛果芸香碱诱导的RHS(半数抑制剂量=0.5纳克),甲溴东莨菪碱不能完全阻断RHS,而RS 86既不产生也不阻断RHS。这些数据(1)利用这一体内终点区分了三种毒蕈碱剂,(2)证实了结合研究将苯海索和甲溴东莨菪碱分别表征为假定的M2和M2拮抗剂,(3)进一步支持使用RHS来研究毒蕈碱剂。