| Identification | Back Directory | [Name]
S-Facinicline | [CAS]
677305-02-1 | [Synonyms]
S-Facinicline
Facinicline hydrochloride | [Molecular Formula]
C15H19ClN4O | [MDL Number]
MFCD32690070 | [MOL File]
677305-02-1.mol | [Molecular Weight]
306.791 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 125 mg/mL (407.44 mM); Methanol: 25 mg/mL (81.49 mM) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active partial agonist of the nicotinic α7 receptor with a Ki of 6 nM for human nAChR. It (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride has a Ki value of 1.2 nM for the 5-HT3 receptor (antagonist). | [in vitro]
Facinicline (RG3487) activates human α7 nAChRs with an EC 50 of 0.8 μM (oocytes) and 7.7 μM (QM7 cells).
It (RG3487) exhibits antagonist properties at the serotonin 3 receptor (IC 50 2.8 nM (oocytes), 32.7 nM (N1E-115 cells)).
< /p> | [in vivo]
Facinicline (RG3487) improves object recognition memory in rats after acute [minimally effective dose (MED) 1.0 mg/kg po] or repeated (10 day) administration at brain and plasma concentrations in the low-nanomolar range.
RG3487 (0.1–10 mg/kg po) selectively enhances object recognition memory.
| Animal Model: | Male Sprague-Dawley rats. | | Dosage: | 0.1-10 mg/kg (Pharmacokinetic Analysis ). | | Administration: | Orally. | < td class="col1 fwb"> Result: | The mean C max was typically observed between 0.5 and 4 h. | | [target]
| 5-HT 3 Receptor 1.2 nM (Ki) | α7 < span> 6 nM (Ki) | | [IC 50]
5-HT3 Receptor: 1.2 nM (Ki); α7: 6 nM (Ki) | [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. DOI:10.1124/jpet.110.171892 |
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