Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rivanicline is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM). It show < 1,000 fold selectivity than α7 receptors(Ki= 36000 nM and IC50 : 26 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | Rivanicline is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM). It show > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM and IC50 : 26 nM). |
In vitro | 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. 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 [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. 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 [2][3]. |
Synonyms | RJR-2403, (E)-Metanicotine |
Molecular Weight | 162.23 |
Formula | C10H14N2 |
CAS No. | 15585-43-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Rivanicline 15585-43-0 Others Metanicotine RJR-2403 (E)-Metanicotine RJR 2403 RJR2403 inhibitor inhibit