SSR180711 hydrochloride

• CAT Number: I011241
• CAS Number: 446031-79-4
• Molecular Formula: C14H18BrClN2O2
• Molecular Weight: 361.66
• Purity: ≥95%
• Synonyms: (4-bromophenyl) 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate;hydrochloride
• InChI: InChI=1S/C14H17BrN2O2.ClH/c15-11-1-3-13(4-2-11)19-14(18)17-10-9-16-7-5-12(17)6-8-16;/h1-4,12H,5-10H2;1H
• InChIKey: YNBXNVUZXFMNSJ-UHFFFAOYSA-N
• SMILES: C1CN2CCC1N(CC2)C(=O)OC3=CC=C(C=C3)Br.Cl

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[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].
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].

Reference

[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.
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