"目录号: HY-14774
Membrane Transporter/Ion ChannelNeuronal Signaling-
Monepantel 是一种有机驱虫剂，也是nAChR的正调节剂。
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L-Nicotine-PNU-282987-Vinblastine-Carbamoylcholine chloride-PNU-120596-Pancuronium dibromide-Aniracetam-Catharanthine-Varenicline-Hexamethonium Bromide-Vecuronium bromide-GTS-21 dihydrochloride-Tebanicline hydrochloride-A-867744-Adiphenine hydrochloride-
生物活性
Description
Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
In Vitro
The metallocenyl analogues of monepantel shows nematocidal activity[1]. Monepantel (25 μM) induces accumulation of acidic vacuoles. Ovarian cancer cell lines are highly sensitive to Monepantel with IC50values of 7.2±0.2 μM (OVCAR-3) and 10.5±0.4 μM (A2780). Monepantel (0, 10 and 25 μM) induces autophagosome formation in these cancer cell lines. Monepantel (0, 10 and 25 μM) exhibits a markedly reduced level of punctate staining indicating the suppression of phosphorylated mTOR at Ser2448. Monepantel also decreases the expression of phosphorylated Raptor at Ser792, which is one of the mTORC1 coMonepantelex members[2]. Monepantel (250 μg/mL) leads multiple ABC transporter genes higher transcription in both worm isolates. Larvae exposed to monepantel at 250 μg/mL shows an increased efflux of rhodamine-123 and a proportion of the larval population shows an ability to subsequently tolerate higher concentrations of IVM in migration assays[3].
In Vivo
Monepantel (10 μM) significantly increased all CYP-related activities and CYP3A24 mRNA in?sheep[4].
References
