ivermectin

Ivermectin (MK-933) 是谷氨酸门控氯离子通道激活剂，具有抗寄生虫活性。它特异性抑制Impα β1 介导的核导入，还抑制牛疱疹病毒 1 复制并抑制BoHV-1DNA 聚合酶的核输入。它具有很强的抗病毒活性。它也是P2X4和 α7nAChRs 的正异构效应物。

Ivermectin B1a 是 Avermectin B1a 的一种衍生物，是 Ivermectin 的主要成分。Ivermectin 是广谱的抗寄生虫剂。Ivermectin 也是抗 SARS-CoV-2 COVID-19 的候选药物。

Ivermectin B1a aglycone is an acid degradation product produced by hydrolysis of the disaccharide unit of ivermectin. It can inhibit nematode larval development, but does not cause paralytic activity.

Ivermectin B1a monosaccharide is produced by selective hydrolysis of the terminal saccharide unit of ivermectin. It can inhibit nematode larval development, but does not cause paralytic activity. This compound has been used as a probe to detect some types of ivermectin resistance.

Ivermectin B1b is the minor component . It produces antiparasitic activity by binding to glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization depolarization of the neuron muscle cell, thereby blocking further function.

2,3-Dehydro-3,4-dihydro ivermectin is an analog of ivermectin and an anthelmintic. 2,3-Dehydro-3,4-dihydro ivermectin has activity against L. amazonensis promastigotes and amastigotes ( IC 50 s=13.8 and 3.6 μM, respectively) without inducing cytotoxicity to macrophages ( IC 50 = 65.5 μM).

Deuterated ivermectin B1a

Ivermectin in Acetonitrile (Standard) 是一种可用于分析的标准物质，通常用作 Ivermectin 的研究和分析中参考的标准样品。Ivermectin 是一种抗寄生虫化合物，可用于寄生虫感染。

Doramectin (Dectomax) 是 Ivermectin 的衍生物。它是一种抗寄生虫抗生素。它具有在 NMRI 小鼠感染模型中抗曼氏链球菌作用。

Selamectin (UK-124114) 是半合成的大环内酯，是一种驱虫剂，可增强线虫中谷氨酸和 GABA 门控氯离子通道的开放。它还是抗寄生虫剂，可激活神经元和咽肌中的谷氨酸门控氯离子通道，以预防恶丝虫，淋巴丝虫和线虫感染。它还是 P-糖蛋白底物和抑制剂，IC50为 120 nM。

UK-124114 (Selamectin) 是伊维菌素的大环内酯衍生物，伊维菌素是一种驱虫剂，可增强线虫中谷氨酸和 GABA 门控氯离子通道的开放。在 H. contortus 幼虫发育试验中，赛拉菌素 (0.1 µg ml) 显示出生长抑制作用。