SSR180711 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 (Ki=22 nM；IC50=30 nM) 和人 α7 n-AChRs (Ki=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)。

SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus.

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).

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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Cell Cycle/DNA Damage

AChR

AChR

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446031-79-4

361.66

C14H18BrClN2O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (138.25 mM; 超声助溶 )

Cl.Brc1ccc(OC(=O)N2CCN3CCC2CC3)cc1

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(-20℃)

With Ice Pack

≥ 2 years