Monepantel

"目录号: HY-14774

Membrane Transporter/Ion Channel Neuronal Signaling-

Monepantel 是一种有机驱虫剂，也是nAChR的正调节剂。

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

[1].Hess J, et al. Assessment of the nematocidal activity of metallocenyl analogues of monepantel. Dalton Trans. 2016 Nov 28;45(44):17662-17671.

[2].Bahrami F, et al. Monepantel induces autophagy in human ovarian cancer cells through disruption of the mTOR/p70S6K signalling pathway. Am J Cancer Res. 2014 Sep 6;4(5):558-71.

[3].Raza A, et al. Increased expression of ATP binding cassette transporter genes following exposure of Haemonchus contortus larvae to a high concentration of monepantel in vitro. Parasit Vectors. 2016 Sep 29;9(1):522.

[4].Stuchlikova, et al. Monepantel induces hepatic cytochromes p450 in sheep in vitro and in vivo. Chem Biol Interact. 2015 Feb 5;227:63-8. ?

Monepantel

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