RJR-2403 - CAS 15585-43-0
Catalog number: 15585-43-0
Category: Inhibitor
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Molecular Formula:
C10H14N2
Molecular Weight:
162.23
COA:
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Targets:
nAChR
Description:
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. 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. 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.
Purity:
>98%
Synonyms:
Rivanicline; Metanicotine; RJR-2403; RJR 2403; RJR2403; Metanicotine; Rivanicline oxalate;
MSDS:
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InChIKey:
JUOSGGQXEBBCJB-GORDUTHDSA-N
InChI:
InChI=1S/C10H14N2/c1-11-7-3-2-5-10-6-4-8-12-9-10/h2,4-6,8-9,11H,3,7H2,1H3/b5-2+
Canonical SMILES:
CNCCC=CC1=CN=CC=C1
1.[Chronic administration of RJR-2403 in combination with low-dose of 17beta-estradiol corrects passive avoidance learning in ovariectomized rats].
Fedotova IuO, Sapronov NS. Eksp Klin Farmakol. 2013;76(5):3-6.
The aim of this work was to study the effect of stimulation or blockade of Na7-cholinoreceptors with a low dose of 17beta-estradiol on the passive avoidance performance and behavior in the open-field test in adult ovariectomized (OVX) female rats. Agonist of Na7-cholinoreceptors RJR-2403 (1.0 mg/kg, i.p.) or antagonist of Na7-cholinoreceptors mecamylamine (1.0 mg/kg, i.p.) treated chronically (14 days) alone and in a combination with low dose of 17beta-estradiol (0.5 microg/rat, s.c.) to OVX rats. Co-administration of RJR-2403 with low dose of 17P-estradiol completely restored impaired passive avoidance performance in OVX females. OVX rats treated with RJR-2403 and low dose of 17beta-estradiol demonstrated increased exploratory and grooming behavior in the open-field test. Both mecamylamine alone and in combination with low dose of 17beta-estradiol failed to influence the passive avoidance learning and failed to modify behavior in the open-field test in OVX rats.
2.[Co-administration of RJR-2403 with low dose of 17beta-estradiol on spatial learning in ovariectomized rats].
Fedotova YO. Patol Fiziol Eksp Ter. 2013 Jul-Sep;(3):37-41.
The aim of this work was to study the influence of stimulation or blockade Nalpha7-cholinoreceptors on dynamics of spatial learning in water Morris maze and on behavior in the "open field" test in adult ovariectomized (OVX) females given with a low dose of 17beta-estradiol. Agonist of Nalpha7-cholinoreceptors - RJR-2403 (1.0 mg/kg, i.p.) or antagonist of Nalpha7-cholinoreceptors - mecamylamine (1.0 mg/kg, i.p.) treated chronically (14 days) alone and in a combination with low dose of 17beta-estradiol (0.5 micro/rat, s.c.) to OVX rats. Co-administration of RJR-2403 with low dose of 17beta-estradiol completely restored impaired spatial learning in water Morris maze in OVX females. Moreover, OVX rats treated with RJR-2403 and low dose of 17beta-estradiol demonstrated increased exploratory and grooming behavior in the "open field" test. Both mecamylamine alone and in combination with low dose of 17beta-estradiol failed to influence on spatial learning and failed to modify behavior in the "open field" test in OVX rats.
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CAS 15585-43-0 RJR-2403

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