Rivanicline
Based on 1 publication(s) in Google Scholar
Rivanicline (RJR-2403) is a neuronal nicotinic receptor agonist. Rivanicline is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline can significantly restore the learning impairment and cognitive dysfunction. Rivanicline can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease).
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- CAS 番号: 15585-43-0
- 分子式: C10H14N2
- 分子量:162.23
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Rivanicline
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生物活性
製品説明
IC50 & Target
[3]|
α4β2 16 μM (EC50) |
α4β4 50 μM (EC50) |
α3β2 150 μM (EC50) |
α7 240 μM (EC50) |
α3β2α5 360 μM (EC50) |
α3β4 NA μM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PC-12 | EC50 |
>1000 μM
Compound: 15
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Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor subtype PC12 (ganglionic)
Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor subtype PC12 (ganglionic)
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[PMID: 9435889] |
体内実験
Rivanicline (75-125 µmol/kg, s.c., single dose) can cause a decrease in body temperature, respiratory rate, Y-maze activity and auditory startle response, but its potency is significantly lower than that of nicotine in mice physiological test battery model[2].
Rivanicline (2 mg/kg, i.p., single dose) restores the learning ability of mice in impairment of eyeblink conditioning model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Scopolamine (1.3 μmol/kg) -induced passive amnesia model established in male wistar rats (200-220 g)[2]
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Dosage:0.06, 0.6, 6 µmol/kg
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Administration:Subcutaneous Injections (s.c.), 30 min before testing
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Result:Reversed scopolamine-induced amnesia, increasing step-through latency at 0.6 µmol/kg.
No effect at 0.06 or 6 µmol/kg.
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Animal Model:Ibotenic acid lesion radial arm maze model established in male Sprague-Dawley rats (250–270 g) [2]
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Dosage:0, 0.3, 0.6, 0.9, 1.2 µmol/kg
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Administration:Subcutaneous Injections (s.c.), 20 min before testing
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Result:Improved working memory (place task) in lesioned rats.
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Animal Model:Physiological test battery model established in C57BL/6 mice[2]
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Dosage:75, 100 and 125 µmol/kg
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Administration:Subcutaneous Injections (s.c.), single dose
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Result:Was 15-50x less potent than nicotine in reducing body temperature, respiration, and locomotor activity.
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Animal Model:MK-801 (0.02 mg/kg)-induced impairment of eyeblink conditioning model established in C57Bl/6 mice (3-5 months)[4]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Rescues learning by activating presynaptic nAChRs to enhance glutamate release.
化学情報
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CAS 番号 15585-43-0
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分子量 162.23
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分子式 C10H14N2
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SMILES
CNCC/C=C/C1=CC=CN=C1
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別名
RJR-2403; (E)-Metanicotine
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
α4 nicotinic receptors on GABAergic neurons mediate a cholinergic analgesic circuit in the substantia nigra pars reticulata. [Abstract]2024 Jun;45(6):1160-1174. PMID: 38438581
純度とドキュメンテーション
参考文献
[1]. Bencherif M, et al. RJR-2403: a nicotinic agonist with CNS selectivity I. In vitro characterization. J Pharmacol Exp Ther. 1996 Dec;279(3):1413-21. [Content Brief]
[2]. Lippiello PM, et al. RJR-2403: a nicotinic agonist with CNS selectivity II. In vivo characterization. J Pharmacol Exp Ther. 1996 Dec;279(3):1422-9. [Content Brief]
[3]. Papke RL, et al The activation and inhibition of human nicotinic acetylcholine receptor by RJR-2403 indicate a selectivity for the alpha4beta2 receptor subtype. J Neurochem. 2000 Jul;75(1):204-16. [Content Brief]
[4]. Rodríguez-Moreno A, et al. The nicotinic agonist RJR-2403 compensates the impairment of eyeblink conditioning produced by the noncompetitive NMDA-receptor antagonist MK-801. Neurosci Lett. 2006 Jul 10;402(1-2):102-7. [Content Brief]
[5]. Damaj MI, et al. Antinociceptive and pharmacological effects of metanicotine, a selective nicotinic agonist. J Pharmacol Exp Ther. 1999 Oct;291(1):390-8. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Rivanicline 関連分類
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