BETA(编程语言)
阿尔法(金融)
受体
烟碱拮抗剂
生物
内分泌学
烟碱激动剂
内科学
生物化学
医学
结构效度
护理部
计算机科学
患者满意度
程序设计语言
作者
Scott C. Harvey,Floyd N. Maddox,Charles W. Luetje
标识
DOI:10.1046/j.1471-4159.1996.67051953.x
摘要
Abstract: Neuronal nicotinic acetylcholine receptors are differentially sensitive to blockade by the competitive antagonist dihydro‐β‐erythroidine. Both α and β subunits participate in determining sensitivity to this antagonist. The α subunit contribution to dihydro‐β‐erythroidine sensitivity is illustrated by comparing the α4β4 receptor and the α3β4 receptor, which differ in sensitivity to dihydro‐β‐erythroidine by ∼120‐fold. IC 50 values for blocking α4β4 and α3β4, responding to EC 20 concentrations of acetylcholine, were 0.19 ± 0.06 and 23.1 ± 10.2 µ M , respectively. To map the sequence segments responsible for this difference, we constructed a series of chimeric α subunits containing portions of the α4 and α3 subunits. These chimeras were coexpressed with β4, allowing pharmacological characterization. We found determinants of dihydro‐β‐erythroidine sensitivity to be distributed throughout the N‐terminal extracellular domain of the α subunit. These determinants were localized to sequence segments 1–94, 94–152, and 195–215. Loss of determinants within segment 1–94 had the largest effect, decreasing dihydro‐β‐erythroidine sensitivity by 4.3‐fold.
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