2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. Rivanicline hydrochloride

Rivanicline hydrochloride  (Synonyms: RJR-2403 hydrochloride; Metanicotine hydrochloride)

Cat. No.: HY-13225H
Handling Instructions Technical Support

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).

For research use only. We do not sell to patients.

Rivanicline hydrochloride Chemical Structure

Rivanicline hydrochloride Chemical Structure

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Description

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)[1][2][3][4][5].

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 (0-1.2 µmol/kg, s.c., single dose) significantly improves passive avoidance retention after scopolamine (HY-N0296) -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[2].
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.

Animal Model: Scopolamine (1.3 μmol/kg) -induced passive amnesia model established in male wistar rats (200-220 g)[2]
Dosage: 0.06, 0.6, 6 µmol/kg
Administration: Subcutaneous Injections (s.c.), 30 min before testing
Result: Reversed scopolamine-induced amnesia, increasing step-through latency at 0.6 µmol/kg.
No effect at 0.06 or 6 µmol/kg.
Animal Model: Ibotenic acid lesion radial arm maze model established in male Sprague-Dawley rats (250–270 g) [2]
Dosage: 0, 0.3, 0.6, 0.9, 1.2 µmol/kg
Administration: Subcutaneous Injections (s.c.), 20 min before testing
Result: Improved working memory (place task) in lesioned rats.
Animal Model: Physiological test battery model established in C57BL/6 mice[2]
Dosage: 75, 100 and 125 µmol/kg
Administration: Subcutaneous Injections (s.c.), single dose
Result: Was 15-50x less potent than nicotine in reducing body temperature, respiration, and locomotor activity.
Animal Model: MK-801 (0.02 mg/kg)-induced impairment of eyeblink conditioning model established in C57Bl/6 mice (3-5 months)[4]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Rescues learning by activating presynaptic nAChRs to enhance glutamate release.
Molecular Weight

198.69

Formula

C10H15ClN2
SMILES

CNCC/C=C/C1=CN=CC=C1.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Rivanicline hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RivaniclineRJR-2403MetanicotineRJR2403RJR 2403nAChRNicotinic acetylcholine receptorsHippocampusEyeblinkClassical conditioningNMDA receptorsNicotinic receptorsPaired-pulse facilitationMiceInhibitorinhibitorinhibit

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