677305-02-1

677305-02-1 structure
677305-02-1 structure
  • Name: Facinicline hydrochloride
  • Chemical Name: Facinicline hydrochloride
  • CAS Number: 677305-02-1
  • Molecular Formula: C15H19ClN4O
  • Molecular Weight: 306.79
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2020-08-11 10:13:01
  • Modify Date: 2024-01-09 16:26:14
  • 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].

Name Facinicline hydrochloride
Description 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].
Related Catalog
Target

5-HT3 Receptor:1.2 nM (Ki)

α7:6 nM (Ki)

In Vitro 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].
In Vivo 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]. Animal Model: Male Sprague-Dawley rats[1]. Dosage: 0.1-10 mg/kg (Pharmacokinetic Analysis). Administration: Orally. Result: The mean Cmax was typically observed between 0.5 and 4 h.
References

[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.

Molecular Formula C15H19ClN4O
Molecular Weight 306.79