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编 号:F423768
分子式:C15H19ClN4O
分子量:306.79
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性:
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.

体内研究:
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.Animal Model:Male Sprague-Dawley rats.
Dosage:0.1-10 mg/kg (Pharmacokinetic Analysis).
Administration:Orally.
Result:The mean Cmax was typically observed between 0.5 and 4 h.

体外研究:
Facinicline (RG3487) activates human α7 nAChRs with an EC50 of 0.8 μM (oocytes) and 7.7 μM (QM7 cells).Facinicline (RG3487) exhibits antagonist properties at the serotonin 3 receptor (IC50 2.8 nM (oocytes), 32.7 nM (N1E-115 cells)).
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