Name | Facinicline hydrochloride |
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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]. |
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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 |
Molecular Formula | C15H19ClN4O |
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Molecular Weight | 306.79 |