Facinicline hydrochloride

• CAT Number: I015399
• CAS Number: 677305-02-1
• Molecular Formula: C15H19ClN4O
• Molecular Weight: 306.79
• Purity: ≥95%
• Synonyms: N-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-1H-indazole-3-carboxamide;hydrochloride
• InChI: InChI=1S/C15H18N4O.ClH/c20-15(14-11-3-1-2-4-12(11)17-18-14)16-13-9-19-7-5-10(13)6-8-19;/h1-4,10,13H,5-9H2,(H,16,20)(H,17,18);1H/t13-;/m1./s1
• InChIKey: CMRLNEYJEPELSM-BTQNPOSSSA-N
• SMILES: C1CN2CCC1C(C2)NC(=O)C3=NNC4=CC=CC=C43.Cl

Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM[1].
Facinicline (RG3487) activates human α7 nAChRs with an EC50 of 0.8 μM (oocytes) and 7.7 μM (QM7 cells)[1].
Facinicline (RG3487) exhibits antagonist properties at the serotonin 3 receptor (IC50 2.8 nM (oocytes), 32.7 nM (N1E-115 cells))[1].
Facinicline (RG3487) improves object recognition memory in rats after acute [minimally effective dose (MED) 1.0 mg/kg p.o.] or repeated (10 day) administration at brain and plasma concentrations in the low-nanomolar range[1].
RG3487 (0.1–10 mg/kg p.o.) selectively enhances object recognition memory[1].

Reference

[1]. Tanya L Wallace, et al. RG3487, a Novel Nicotinic α7 Receptor Partial Agonist, Improves Cognition and Sensorimotor Gating in Rodents. J Pharmacol Exp Ther. 2011 Jan;336(1):242-53.
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