SSR180711 盐酸盐

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 (IC ₅₀ >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 EC ₅₀ value of 4.4 μM (2.5-7.8 μM).

SSR180711 hydrochloride rapidly penetrates into the brain (ID ₅₀ =8 mg/kg; p.o.). SSR180711 hydrochloride dose-dependently inhibits the specific [ ^3H ]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.