Rivanicline oxalate  (Synonyms: RJR-2403 oxalate; (E)-Metanicotine oxalate)

Rivanicline (RJR-2403) oxalate is a neuronal nicotinic receptor agonist. Rivanicline oxalate is highly selective for the rat brain cortex nAChRs (K_i = 26 nM, EC₅₀ of 732 nM) and α4β2 subtype (K_i = 26 nM, EC₅₀ = 16 μM). Rivanicline oxalate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline oxalate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease)^{[1][2][3][4][5]}.

Rivanicline oxalate (0-1.2 µmol/kg, s.c., single dose) significantly improves passive avoidance retention after scopolamine (HY-N0296) -induced amnesia and enhanced both working and reference memory in rats with ibotenic acid lesions of the forebrain cholinergic projection system in an 8-arm radial maze^[2].
Rivanicline oxalate (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 oxalate (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.

252.27

C₁₂H₁₆N₂O₄

220662-95-3

CNCC/C=C/C1=CC=CN=C1.OC(C(O)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]