【摘要】：目的:比較α和β亞基不同配比形成α3β2和α3β4煙堿型乙酰膽堿受體(nAChR)敏感性的差異。方法:體外轉(zhuǎn)錄獲得α和β亞基的cRNA,采用顯微注射將3種不同配比(α∶β分別為1∶10、1∶1和10∶1)的cRNA注入非洲爪蟾卵母細(xì)胞,利用雙電極電壓鉗檢測受體表達(dá)情況。利用激動劑乙酰膽堿(ACh)和拮抗劑α-芋螺毒素Reg IIA(α-CTx Reg IIA)檢測在3種配比條件下形成受體藥理活性的差異。結(jié)果:對于α3β2 nAChR亞型,在3種配比情況下,ACh的半數(shù)有效濃度(EC50)分別為91.2μmol/L、104.4μmol/L和130.6μmol/L,α-CTx Reg IIA的半數(shù)抑制濃度(IC50)分別為40.2 nmol/L、36.4 nmol/L和42.3 nmol/L。對于α3β4 nAChR亞型,在3種配比情況下,ACh的EC50分別為44.0μmol/L、110.0μmol/L和230.0μmol/L,α-CTx Reg IIA的IC50分別為226.8 nmol/L、71.5 nmol/L和49.4 nmol/L。結(jié)論:α3和β4亞基比例的改變會導(dǎo)致α3β4 nAChR結(jié)構(gòu)和藥理活性的改變。α3和β2亞基比例的改變對α3β2 nAChR結(jié)構(gòu)和活性沒有影響。
[Abstract]:Aim: to compare the sensitivity of 偽 3 尾 2 and 偽 3 尾 4 nicotinic acetylcholine receptor (nAChR) to 偽 3 尾 2 and 偽 3 尾 subunits. Methods: cRNA, of 偽 and 尾 subunits obtained by transcription in vitro were injected into Xenopus laevis oocytes with three different ratios (偽: 尾 = 1: 10: 1: 1: 1 and 10:1) by microinjection. The expression of receptor was detected by double electrode voltage clamp. Agonist acetylcholine (ACh) and antagonist 偽 -Conotoxin Reg IIA (偽 CTx Reg IIA) were used to detect the difference of pharmacological activity of the receptors formed under three conditions. Results: for 偽 3 尾 2 nAChR subtype, the half effective concentration (EC50) of ACh was 91.2 渭 mol/L,104.4 渭 mol/L and 130.6 渭 mol/L, 偽 -CTx Reg IIA was 40.2 nmol/L, respectively. 36.4 nmol/L and 42.3 nmol/L. For 偽 3 尾 4 nAChR subtype, the EC50 of ACh is 44.0 渭 mol/L,110.0 渭 mol/L and 230.0 渭 mol/L, 偽 -CTx Reg IIA IC50 is 226.8 nmol/L,71.5 nmol/L and 49.4 nmol/L., respectively. Conclusion: the ratio of 偽 3 and 尾 4 subunits may lead to the change of the structure and pharmacological activity of 偽 3 尾 4 nAChR, but the ratio of 偽 3 and 尾 2 subunits has no effect on the structure and activity of 偽 3 尾 2 nAChR.
【作者單位】： 海南大學(xué)熱帶生物資源教育部重點(diǎn)實(shí)驗(yàn)室�？谑泻Ｑ笏幬镏攸c(diǎn)實(shí)驗(yàn)室海洋學(xué)院藥學(xué)系;
【基金】：國家自然科學(xué)基金重點(diǎn)國際合作項(xiàng)目(No.81420108028);國家自然科學(xué)基金資助項(xiàng)目(No.41366002) 長江學(xué)者和創(chuàng)新團(tuán)隊(duì)發(fā)展計劃項(xiàng)目(No.IRT-15R15) 海南省高等學(xué)�？茖W(xué)研究項(xiàng)目(No.Hnky2017-16) 海南大學(xué)科研啟動基金資助項(xiàng)目[No.KYQD(ZR)1713
【分類號】：R96

【相似文獻(xiàn)】

相關(guān)期刊論文 前1條

1 黎淵弘;林文珍;臧寧;梁瑩;黎肇炎;;短尾蝮蛇毒磷脂結(jié)合抗凝蛋白β亞基的基因克隆和序列分析[J];廣西醫(yī)科大學(xué)學(xué)報;2010年02期

，

本文編號：2403022