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Rivanicline

Catalog No. T12738L   CAS 15585-43-0
Synonyms: RJR-2403, (E)-Metanicotine

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).

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Rivanicline Chemical Structure
Rivanicline, CAS 15585-43-0
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
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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. 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. 3. Damaj MI, et al. Antinociceptive and pharmacological effects of metanicotine, a selective nicotinic agonist. J Pharmacol Exp Ther. 1999 Oct;291(1):390-8.

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Keywords

Rivanicline 15585-43-0 Others Metanicotine RJR-2403 (E)-Metanicotine RJR 2403 RJR2403 inhibitor inhibit

 

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