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Nematode Cholinergic Receptors as Drug Targets; Recent Findings and Potential Implications

机译:Nematode Cholinergic受体作为药物目标;最近的发现和潜在的影响

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Cholinergic anthelmintics belong to several different chemical classes. Recent observations on the C. elegans genome and pharmacology of Ascaris suum muscle strips show that the action of cholinergic drugs is not on a single homogenous population of acetylcholine receptors. In this paper we describe single-channel studies that separate out: 1) a nicotine-preferring, N-subtype, that has a conductance of 25 pS; 2) a levamisole-preferring, L-subtype, that has a conductance of 35 pS; and 3) a bephenium-preferring, B-subtype, has a conductance of 45 pS. In larval migration assays, levamisole-resistant isolates are less sensitive to levamisole & pyrantel but not less sensitive to methyridine & nicotine, suggesting that combinations of cholinergic anthelmintics may overcome some types of resistance.
机译:Cholinergic Anthelmintics属于几种不同的化学类别。最近对伊育杆菌基因组和药理学的观察结果表明,胆碱能药物的作用不是在单一的乙酰胆碱受体群体上。在本文中,我们描述了单一的单通道研究,分离出:1)尼古丁霍尔的N-Subtype,其具有25 ps的电导; 2)Levamisole偏好的L-亚型,具有35 ps的电导; 3)苯甲酸苯甲酸苯甲酸亚型,具有45ps的电导率。在幼虫迁移测定中,左旋咪唑抗性分离物对左旋吲哚和吡喃酮,但对甲甲醇和尼古丁的敏感性不太敏感,这表明胆碱能结构的组合可以克服某种类型的抗性。

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