RJR-2403
Modify Date: 2024-01-07 11:32:12
RJR-2403 structure
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Common Name | RJR-2403 | ||
|---|---|---|---|---|
| CAS Number | 15585-43-0 | Molecular Weight | 162.23200 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C10H14N2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of RJR-2403Rivanicline (RJR-2403) 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).IC50 value: 26 nM [1]Target: α4β2 nAChRin vitro: At concentrations up to 1 mM, Rivanicline does not significantly activate nAChRs in PC12 cells, muscle type nAChRs or muscarinic receptors. Dose-response curves for agonist-induced ileum contraction indicate that Rivanicline is less than one-tenth as potent as nicotine with greatly reduced efficacy. Rivanicline does not antagonize nicotine-stimulated muscle or ganglionic nAChR function (IC50 > 1 mM). Chronic exposure of M10 cells to Rivanicline (10 microM) results in an up-regulation of high-affinity nAChRs phenomenologically similar to that seen with nicotine [1].in vivo: Rivanicline 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, Rivanicline 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]. |
| Name | (3E)-N-Methyl-4-(3-pyridinyl)-3-buten-1-amine |
|---|---|
| Synonym | More Synonyms |
| Description | Rivanicline (RJR-2403) 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).IC50 value: 26 nM [1]Target: α4β2 nAChRin vitro: At concentrations up to 1 mM, Rivanicline does not significantly activate nAChRs in PC12 cells, muscle type nAChRs or muscarinic receptors. Dose-response curves for agonist-induced ileum contraction indicate that Rivanicline is less than one-tenth as potent as nicotine with greatly reduced efficacy. Rivanicline does not antagonize nicotine-stimulated muscle or ganglionic nAChR function (IC50 > 1 mM). Chronic exposure of M10 cells to Rivanicline (10 microM) results in an up-regulation of high-affinity nAChRs phenomenologically similar to that seen with nicotine [1].in vivo: Rivanicline 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, Rivanicline 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]. |
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| Related Catalog | |
| References |
| Molecular Formula | C10H14N2 |
|---|---|
| Molecular Weight | 162.23200 |
| Exact Mass | 162.11600 |
| PSA | 24.92000 |
| LogP | 2.09520 |
| Storage condition | 2-8℃ |
| (E)-N-methyl-4-(3-pyridinyl)-3-butene-1-amine |
| (E)-N-methyl-4-(3-(pyridin)yl)-3-buten-1-amine |
| trans-metanicotine |
| ritodrine(erythro) |
| Metanicotin |
| Rivanicline |
| RJR-2403 |