摘要
放射受体结合试验表明脑桥、延髓存在M_1受体(约30～40％)和M_2受体(约60～70％);皮层海马M_1受体为主(约90％),小脑为M_2受体。东莨菪碱对皮层海马M_1受体的亲和力是小脑M_2受体亲和力的22.72倍,阿托品对小脑M_2受体亲和力是对皮层海马M_1受体亲和力的3.89倍。结果提示东莨菪碱、阿托品分别对M_1、M_2受体有一定的选择性。
Radioligand binding experiments using 3H-QNB and 3H-PZ were Performed on the cortex and hippocampus, Pons, medulla oblongata and cerebellum of Wistar rat brains. It was found that the M1 cholinergic recePtor accounted for approximately 90% the total muscarinic receptors in the cortex and hiPPo-camPus, and the M2 accounted for only about 10%. In the Pons and medulla oblongata, the MI cholinergic receptor accounted for appoximately 30-40% the total muscarinic receptors in these 2 brain parts; and the M2 accounted for about 60-70%. When separate scoPolamine , atro,Pine , pirenzePine and AF-DX 116 were added to comPete against the 3H- labelled reagents in binding to the receptors in the four parts of brain, the Pki values obtained showed that the affinities of scoPolamine and PirenzePine for cortex-hiPPocamp-us ( Ml ) were 22.7 and 303.3 times higher than those for cerebellum ( M2 ) . The affinities of AF-DX 116 and atropine for cerebellum were respectively 31.6 times and 3.89 times higher than those for cortex-hiPPocamPus . These results suggest that scoPolamine has higher selectivity for the M1 than for the Mi, while the selectivity of atroPine is higher for the M2 than the M1.
出处
《徐州医学院学报》
CAS
1991年第1期5-11,共7页
Acta Academiae Medicinae Xuzhou
关键词
脑干
M受体
亚型
药物
muscarinic receptor subtype
radioligand binding experiment, PirenzePine
AF-DX 116
scopolamine
atroPine
rats
