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SSR180711 hydrochloride

CAS No. : 446031-79-4

MCE 站：SSR180711 hydrochloride

产品活性：SSR180711 hydrochloride 是具有口服活性，选择性和可逆的 α7 n-AChRs 部分激动剂。SSR180711 hydrochloride 可以作用于大鼠 α7 n-AChRs (K_i=22 nM；IC₅₀=30 nM) 和人 α7 n-AChRs (K_i=14 nM；IC₅₀=18 nM)。SSR180711 hydrochloride 增加海马区的谷氨酸能神经传递，Ach 释放和长时程增强 (LTP)。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：nAChR

In Vitro: SSR180711 hydrochloride is selective for the α7 receptor subtype compared to α4β2, α3β2, α3β4, and α1β1γδ human n-AChR subtypes (IC₅₀>5?μM). SSR180711 hydrochloride (10?μM) has no inhibition (lower than 50%) for the ionic channels, neurotransmitter, or peptide receptors.
SSR180711 hydrochloride (0.01-10000 μM) is a potent partial agonist at human α7 n-AChRs expressed in Xenopus oocytes or GH4C1 cells and elicits typical concentration-dependent inward currents with an EC₅₀ value of 4.4?μM (2.5-7.8?μM).

In Vivo: SSR180711 hydrochloride rapidly penetrates into the brain (ID₅₀=8?mg/kg; p.o.). SSR180711 hydrochloride dose-dependently inhibits the specific [^3H]α-BTX binding in the mouse brain (ID₅₀=8.3 and 7.5?mg/kg for p.o. and i.p., respectively).
SSR180711 hydrochloride (1-10?mg/kg for i.p.; 10-30 mg/kg for p.o.) dose-dependently increases extracellular acetylcholine (ACh) levels in the hippocampus and prefrontal cortex of freely moving rats.
SSR180711 hydrochloride (0.1, 0.3, 1?mg/kg; i.v.) dose-dependently increases firing rate.

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