Facinicline hydrochloride

Modify Date: 2024-01-09 16:26:14

Facinicline hydrochloride Structure
Facinicline hydrochloride structure
Common Name Facinicline hydrochloride
CAS Number 677305-02-1 Molecular Weight 306.79
Density N/A Boiling Point N/A
Molecular Formula C15H19ClN4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Facinicline hydrochloride


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].

 Names

Name Facinicline hydrochloride

 Facinicline hydrochloride Biological Activity

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.

 Chemical & Physical Properties

Molecular Formula C15H19ClN4O
Molecular Weight 306.79
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