Rivanicline fumarate
Rivanicline (RJR-2403) fumarate is a neuronal nicotinic receptor agonist. Rivanicline fumarate 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 fumarate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline fumarate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease).
For research use only. We do not sell to patients.
- CAS No.: 183288-99-5
- Formula: C14H18N2O4
- Molecular Weight:278.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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α4β2 16 μM (EC50) |
α4β4 50 μM (EC50) |
α3β2 150 μM (EC50) |
α7 240 μM (EC50) |
α3β2α5 360 μM (EC50) |
α3β4 NA μM (EC50) |
Rivanicline fumarate (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 fumarate (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.
Chemical Information
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CAS No. 183288-99-5
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Molecular Weight 278.30
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Formula C14H18N2O4
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SMILES
CNCC/C=C/C1=CC=CN=C1.O=C(O)/C=C/C(O)=O
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Synonyms
RJR-2403 fumarate; (E)-Metanicotine fumarate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Rivanicline fumarate Related Classifications
HY-13225D Related Classifications
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