For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>RJR-2403(Metanicotine; Rivanicline) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM).<br>IC50 value: 26 nM [1]<br>Target: α4β2 nAChR<br>in vitro: At concentrations up to 1 mM, RJR-2403 does not significantly activate nAChRs in PC12 cells, muscle type nAChRs or muscarinic receptors. Dose-response curves for agonist-induced ileum contraction indicate that RJR-2403 is less than one-tenth as potent as nicotine with greatly reduced efficacy. RJR-2403 does not antagonize nicotine-stimulated muscle or ganglionic nAChR function (IC50 > 1 mM). Chronic exposure of M10 cells to RJR-2403 (10 microM) results in an up-regulation of high-affinity nAChRs phenomenologically similar to that seen with nicotine [1].<br>in vivo: RJR-2403 significantly improved passive avoidance retention after scopolamine-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 paradigm. By comparison, RJR-2403 was 15 to 30-fold less potent than nicotine in decreasing body temperature, respiration, Y-maze rears and crosses and acoustic startle response [2]. Metanicotine was about 5-fold less potent than nicotine in the tail-flick test after s.c administration, but slightly more potent after central administration [3].</p>
| Catalog Number | I001978 |
| CAS Number | 15585-43-0 |
| Synonyms | (E)-N-methyl-4-pyridin-3-ylbut-3-en-1-amine |
| Molecular Formula | C10H14N2 |
| Purity | ≥95% |
| Target | Neuronal Signaling |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| IC50 | 26 nM [1] |
| Reference | <p style=/line-height:25px/> |
