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采用放射配基与受体结合实验,研究了烟碱对M受体亲和力的影响.结果表明35℃下烟碱1.0μmol·L_(-1)与大鼠脑匀浆温育30min,M激动剂槟榔碱及氧化震颤素与mAChR高亲和力结合位点的亲和力显著增强,Kd值分别由0.35±0.11(n=5)降至0.03±0.01(n=7)μmol·L_(-1),P<0.01;由7.00±3.95(n=3)降至0.48±0.44(n=4)P<0.05;而与低亲和力位点的亲和力及高、低亲和力位点的比例无显著变化,烟碱与脑匀浆温育30min后,M拮抗剂QNB与mAChR结合的亲和力显著降低,0.1 nmol·L~(-1)10μmol·L_(-1)烟碱浓度依赖性
The effects of nicotine on the affinity of M receptor were studied by the combination of radioligand and receptor.The results showed that nicotine 1.0 μmol·L_ (-1) incubated with rat brain homogenate at 35 ℃ for 30 min, M agonist The affinity of arecoline and oxotremorine to mAChR high affinity binding sites was significantly enhanced, with Kd values decreasing from 0.35 ± 0.11 (n = 5) to 0.03 ± 0.01 (n = 7) μmol·L_ (-1), P < (P <0.05). However, there was no significant change in the affinity with low affinity sites and the ratio of high and low affinity sites, and nicotine and brain decreased significantly from 7.00 ± 3.95 (n = 3) to 0.48 ± 0.44 The affinity of MNB antagonist QNB and mAChR was significantly reduced after incubation for 30 min, and the concentration dependence of 0.1 nmol·L -1 10 μmol·L -1 nicotine