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)。

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 (K i =22 nM; IC 50 =30 nM) and human α7 n-AChR (K i =14 nM; IC 50 =18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus.

Solid

IC50: 30 nM (rat α7 n-AChR) and 18 nM (human α7 n-AChR)
Ki: 22 nM (rat α7 n-AChR) and 14 nM (human α7 n-AChR)

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).
has not independently confirmed the accuracy of these methods. They are for reference only.

SSR180711 hydrochloride rapidly penetrates into the brain (ID 50 =8?mg/kg; p.o.). SSR180711 hydrochloride dose-dependently inhibits the specific []α-BTX binding in the mouse brain (ID 50 =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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Bruno Biton, et al. SSR180711, a novel selective alpha7 nicotinic receptor partial agonist: (1) binding and functional profile. Neuropsychopharmacology. 2007 Jan;32(1):1-16.

In Vitro: DMSO : 50 mg/mL (138.25 mM; Need ultrasonic)配制储备液