|RJR-2403 Nicotinic receptor agonist,highly selective|
Sample solution is provided at 25 µL, 10mM.
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|Description||RJR-2403 is an agonist of neuronal nicotinic receptor with Ki value of 26 nM for α4β2 receptor.|
|Targets||α4β2 nicotinic receptor|
|IC50||26 nM (Ki)|
|Cas No.||15585-43-0||SDF||Download SDF|
|Synonyms||Rivanicline; Metanicotine; RJR 2403|
|Solubility||Soluble in DMSO||Storage||Store at -20°C|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
Ki: RJR-2403 compound binds with high affinity to [3H]nicotine binding sites in rat brain (Ki 526 nM) but possesses weak affinity (36 mM) for the 125I-labeled a-bungarotoxin-sensitive nAChR subtype .
RJR-2403 (TC-2403, Rivanicline, (E)-metanicotine) is a drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It is subtype-selective, binding primarily to the α4β2 subtype. It has nootropic effects and was originally developed as a potential treatment for Alzheimer's disease, but a second action that was subsequently found was that it inhibits the production of Interleukin-8 and thus produces an antiinflammatory effect, and so it has also been developed as a potential treatment for ulcerative colitis. RJR-2403 also has stimulant and analgesic actions which are thought to be mediated through stimulation of noradrenaline release, and so it could potentially also have other applications.
In vitro: Prevous in vitro results suggest that RJR-2403 interacts with higher potency at CNS nAChR sub-types than at muscle, ganglionic or enteric nAChRs and has higher selectivity for CNS vs. muscle or ganglionic nAChRs than does nicotine. .
In vivo: The data from an in vivo study demonstrate the efficacy of oral RJR 2403 in improving cognitive performance and the long duration of action of RJR 2403 in young adult rats. In contrast, no significant memory improvement was seen in aged rats aged (24–26 months old) after RJR 2403 administration. The inability of RJR 2403 to enhanced cognitive functions in aged rats might be related to the decrease in the number of α4β2 nicotinic receptors, which occurs with age. A similar decreased responsiveness in aged rats has been seen with nicotine. The persistence of action of RJR 2403 provides additional promise for its potential as a treatment for cognitive dysfunction .
Clinical trial: Up to now, RJR-2403 is still in the preclinical development stage.
 Damaj MI, Glassco W, Aceto MD, Martin BR.Antinociceptive and pharmacological effects of metanicotine, a selective nicotinic agonist. J Pharmacol Exp Ther. 1999;291(1):390-8.
 Bencherif M, Lovette ME, Fowler KW, Arrington S, Reeves L, Caldwell WS, Lippiello PM. RJR-2403: a nicotinic agonist with CNS selectivity I. In vitro characterization. J Pharmacol Exp Ther. 1996;279(3):1413-21.
 Edward D. Levin and N. Channelle Christopher. Persistence of nicotinic agonist RJR 2403-induced working memory improvement in rats. Drug Development Research. 55(2):97–103, 2002