SSR180711 hydrochloride 

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; IC₅₀=30 nM) and human α7 n-AChR (K_i=14 nM; IC₅₀=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus^[1].

IC50: 30 nM (rat α7 n-AChR) and 18 nM (human α7 n-AChR)^[1]
Ki: 22 nM (rat α7 n-AChR) and 14 nM (human α7 n-AChR)^[1]

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^[1].
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)^[1].

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

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)^[1].
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^[1].
SSR180711 hydrochloride (0.1, 0.3, 1 mg/kg; i.v.) dose-dependently increases firing rate^[1].

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

361.66

Solid

C₁₄H₁₈BrClN₂O₂

446031-79-4

O=C(N1CCN2CCC1CC2)OC3=CC=C(Br)C=C3.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*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.  [Content Brief]