S-Facinicline
S-Facinicline Basic information
- Product Name:
- S-Facinicline
- Synonyms:
-
- S-Facinicline
- Facinicline hydrochloride
- RG3487
- RG3487 hydrochloride
- Inhibitor,nAChR,serotonin 3 receptor,Nicotinic acetylcholine receptors,Serotonin Receptor,5-HT Receptor,inhibit,recognition,5-hydroxytryptamine Receptor,Facinicline,Facinicline hydrochloride,receptor,RG-3487,memory,RG 3487,nicotinic
- CAS:
- 677305-02-1
- MF:
- C15H19ClN4O
- MW:
- 306.79056
- Mol File:
- 677305-02-1.mol
S-Facinicline Chemical Properties
- 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
S-Facinicline Usage And Synthesis
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)).
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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. |
| 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) |
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