Rivanicline hydrochloride
Based on 1 publication(s) in Google Scholar
Rivanicline (RJR-2403) hydrochloride is a neuronal nicotinic receptor agonist. Rivanicline hydrochloride is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline hydrochloride can significantly restore the learning impairment and cognitive dysfunction. Rivanicline hydrochloride can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease).
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- Formule: C10H15ClN2
- Masse moléculaire:198.69
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Rivanicline hydrochloride
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Activité biologique
Description
IC50 & Target
[3]|
α4β2 16 μM (EC50) |
α4β4 50 μM (EC50) |
α3β2 150 μM (EC50) |
α7 240 μM (EC50) |
α3β2α5 360 μM (EC50) |
α3β4 NA μM (EC50) |
In Vivo
Rivanicline hydrochloride (75-125 µmol/kg, s.c., single dose) can cause a decrease in body temperature, respiratory rate, Y-maze activity and auditory startle response, but its potency is significantly lower than that of nicotine in mice physiological test battery model[2].
Rivanicline hydrochloride (2 mg/kg, i.p., single dose) restores the learning ability of mice in impairment of eyeblink conditioning model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Scopolamine (1.3 μmol/kg) -induced passive amnesia model established in male wistar rats (200-220 g)[2]
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Dosage:0.06, 0.6, 6 µmol/kg
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Administration:Subcutaneous Injections (s.c.), 30 min before testing
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Result:Reversed scopolamine-induced amnesia, increasing step-through latency at 0.6 µmol/kg.
No effect at 0.06 or 6 µmol/kg.
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Animal Model:Ibotenic acid lesion radial arm maze model established in male Sprague-Dawley rats (250–270 g) [2]
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Dosage:0, 0.3, 0.6, 0.9, 1.2 µmol/kg
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Administration:Subcutaneous Injections (s.c.), 20 min before testing
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Result:Improved working memory (place task) in lesioned rats.
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Animal Model:Physiological test battery model established in C57BL/6 mice[2]
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Dosage:75, 100 and 125 µmol/kg
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Administration:Subcutaneous Injections (s.c.), single dose
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Result:Was 15-50x less potent than nicotine in reducing body temperature, respiration, and locomotor activity.
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Animal Model:MK-801 (0.02 mg/kg)-induced impairment of eyeblink conditioning model established in C57Bl/6 mice (3-5 months)[4]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Rescued learning by activating presynaptic nAChRs to enhance glutamate release.
Chemical Information
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Masse moléculaire 198.69
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Formule C10H15ClN2
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SMILES
CNCC/C=C/C1=CN=CC=C1.Cl
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Synonyms
RJR-2403 hydrochloride; Metanicotine hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
α4 nicotinic receptors on GABAergic neurons mediate a cholinergic analgesic circuit in the substantia nigra pars reticulata. [Abstract]2024 Jun;45(6):1160-1174. PMID: 38438581
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
[3]. Papke RL, et al The activation and inhibition of human nicotinic acetylcholine receptor by RJR-2403 indicate a selectivity for the alpha4beta2 receptor subtype. J Neurochem. 2000 Jul;75(1):204-16. [Content Brief]
[4]. Rodríguez-Moreno A, et al. The nicotinic agonist RJR-2403 compensates the impairment of eyeblink conditioning produced by the noncompetitive NMDA-receptor antagonist MK-801. Neurosci Lett. 2006 Jul 10;402(1-2):102-7. [Content Brief]
[5]. Damaj MI, et al. Antinociceptive and pharmacological effects of metanicotine, a selective nicotinic agonist. J Pharmacol Exp Ther. 1999 Oct;291(1):390-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Rivanicline hydrochloride Related Classifications
HY-13225H Related Classifications
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