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Rhosin hydrochloride

CAS No. : 1281870-42-5

MCE 國際站：Rhosin hydrochloride

產(chǎn)品活性：Rhosin hydrochloride 是一種有效的，特異性的 RhoA 亞家族 Rho GTPases 抑制劑，能特異性的結(jié)合 RhoA，抑制 RhoA-GEF 相互作用，K_d 值 ~ 0.4 uM，但不與 Cdc42 或 Rac1，GEF，LARG 相互作用。Rhosin hydrochloride 可誘導(dǎo)細(xì)胞凋亡。Rhosin hydrochloride 通過增強(qiáng) D1 中棘神經(jīng)元的可塑性和降低過度興奮性來促進(jìn)應(yīng)激恢復(fù)。

研究領(lǐng)域：GPCR/G Protein  |  Apoptosis

作用靶點：Ras  |  Apoptosis

In Vitro: Rhosin hydrochloride dose-dependently reduces RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres with an EC₅₀ ~30-50 μM, and causes decreased size and reduced number of mammospheres in MCF7 cells.

In Vivo: Rhosin (40 mg/kg; i.p.) treatment prevents social avoidance caused by social defeat stress. Rhosin also blocks sucrose preference deficits induced by defeat in C57Bl6/J (Jackson) mice.
?Rhosin (30 μM; bilateral, intra- Nucleus Accumbens (NAc) infusions) attenuates stress-induced social avoidance. Rhosin blocks stress-induced hyperexcitability in NAc dopamine 1 receptor medium spiny neurons (D1-MSNs). Rhosin prevents decreased excitatory transmission on NAc D1-MSNs. Rhosin enhances spine density in defeat mice.

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