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9
The ion channel of muscle and electric organ acetylcholine receptors: differing affinities for noncompetitive inhibitors.肌肉和电器官乙酰胆碱受体的离子通道：对非竞争性抑制剂的不同亲和力。
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Multiple affinity states for noncompetitive blockers revealed by [3H]phencyclidine binding to acetylcholine receptor rich membrane fragments from Torpedo marmorata.
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[3H]Phencyclidine: a probe for the ionic channel of the nicotinic receptor.[3H]苯环己哌啶：一种用于烟碱型受体离子通道的探针。
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A simple assay for the study of solubilized acetylcholine receptors.一种用于研究可溶性乙酰胆碱受体的简易测定法。
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Use of chemical modifications and site-directed mutagenesis to probe the functional role of thiol groups on the gamma subunit of Torpedo californica acetylcholine receptor.利用化学修饰和定点诱变来探究加州电鳐乙酰胆碱受体γ亚基上硫醇基团的功能作用。
Biochemistry. 1989 Aug 8;28(16):6562-71. doi: 10.1021/bi00442a006.
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Desensitization of the nicotinic acetylcholine receptor: molecular mechanisms and effect of modulators.烟碱型乙酰胆碱受体的脱敏：分子机制及调节剂的作用
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An analog of lophotoxin reacts covalently with Tyr190 in the alpha-subunit of the nicotinic acetylcholine receptor.
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Nonequivalence of alpha-bungarotoxin binding sites in the native nicotinic receptor molecule.天然烟碱样受体分子中α-银环蛇毒素结合位点的不等效性。
Biochemistry. 1990 Jan 30;29(4):1046-54. doi: 10.1021/bi00456a029.

来自加勒比海柳珊瑚的二萜类化合物可作为烟碱型乙酰胆碱受体的非竞争性抑制剂。

Diterpenoids from Caribbean gorgonians act as noncompetitive inhibitors of the nicotinic acetylcholine receptor.

作者信息

Eterović V A, Hann R M, Ferchmin P A, Rodriguez A D, Li L, Lee Y H, McNamee M G

机构信息

Department of Biochemistry, Universidad Central del Caribe, Bayamón, Puerto Rico 00960.

出版信息

Cell Mol Neurobiol. 1993 Apr;13(2):99-110. doi: 10.1007/BF00735367.

DOI:10.1007/BF00735367
PMID:8102324
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11566958/
Abstract
  1. Three cyclic diterpenoids isolated from gorgonians of the Eunicea genus and characterized as eupalmerin acetate (EUAC), 12,13-bisepieupalmerin (BEEP), and eunicin (EUNI) were found to be pharmacologically active on the nicotinic acetylcholine receptor (AChR). 2. The receptor from the BC3H-1 muscle cell line was expressed in Xenopus laevis oocytes and studied with a two-electrode voltage clamp apparatus. 3. All three compounds reversibly inhibited ACh-induced currents, with IC50's from 6 to 35 microM. ACh dose-response curves suggested that his inhibition was noncompetitive. The cembranoids also increased the rate of receptor desensitization. 4. Radioligand-binding studies using AChR-rich membranes from Torpedo electric organ indicated that all three cembranoids inhibited high-affinity [3H]phencyclidine binding, with IC50's of 0.8, 11.6, and 63.8 microM for EUNI, EUAC, and BEEP, respectively. The cembranoids at a 100 microM concentration did not inhibit [alpha-125I]bungarotoxin binding to either membrane-bound or solubilized AChR. 5. It is concluded that these compounds act as noncompetitive inhibitors of peripheral AChR.
摘要
  1. 从Eunicea属柳珊瑚中分离出的三种环状二萜类化合物，分别鉴定为乙酸尤帕麦灵（EUAC）、12,13-双表尤帕麦灵（BEEP）和尤尼辛（EUNI），被发现对烟碱型乙酰胆碱受体（AChR）具有药理活性。2. BC3H-1肌肉细胞系的受体在非洲爪蟾卵母细胞中表达，并用双电极电压钳装置进行研究。3. 所有这三种化合物均可逆地抑制乙酰胆碱诱导的电流，IC50值在6至35微摩尔之间。乙酰胆碱剂量反应曲线表明这种抑制是非竞争性的。这些西松烷类化合物还提高了受体脱敏的速率。4. 使用电鳐电器官富含AChR的膜进行的放射性配体结合研究表明，所有这三种西松烷类化合物均抑制高亲和力的[3H]苯环利定结合，EUNI、EUAC和BEEP的IC50值分别为0.8、11.6和63.8微摩尔。100微摩尔浓度的西松烷类化合物不抑制[α-125I]银环蛇毒素与膜结合或可溶的AChR的结合。5. 得出的结论是，这些化合物作为外周AChR的非竞争性抑制剂起作用。