15585-43-0
Chemical Structure
Rivanicline
Synonym(s): RJR-2403;(E)-Metanicotine
- CAS No.: 15585-43-0
- Formula:C10H14N2
- Molecular Weight:162.23
IUPAC Name: (E)-N-methyl-4-(pyridin-3-yl)but-3-en-1-amine
InChIKey: JUOSGGQXEBBCJB-GORDUTHDSA-N
SMILES: CNCC/C=C/C1=CC=CN=C1
Biological Activity: 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)[1][2][3][4][5].
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Rivanicline | 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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Rivanicline-d3 | Rivanicline-d3 (RJR-2403-d3) is the deuterium labeled Rivanicline. Rivanicline (RJR-2403) is a neuronal nicotinic receptor agonist.. | |||||||||||||||||||||
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- [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]
Keywords
