Facinicline hydrochloride

Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a K i 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-HT 3 Rs with a K i value of 1.2 nM In Vitro Facinicline (RG3487) activates human α7 nAChRs with an EC 50 of 0.8 μM (oocytes) and 7.7 μM (QM7 cells). Facinicline (RG3487) exhibits antagonist properties at the serotonin 3 receptor (IC 50 2.8 nM (oocytes), 32.7 nM (N1E-115 cells)). MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . RG3487 (0.1–10 mg/kg p.o.) selectively enhances object recognition memory . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats . Dosage: 0.1-10 mg/kg (Pharmacokinetic Analysis). Administration: Orally. Result: The mean C max was typically observed between 0.5 and 4 h. Form:Solid IC50& Target:5-HT 3 Receptor 1.2 nM (Ki) α7 6 nM (Ki)

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