Noribogaine hydrochloride
Based on 1 Customer Validation
Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC50=50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity.
For research use only. We do not sell to patients.
- Purity: 99.9%
- CAS No.: 110514-35-7
- Formula: C19H25ClN2O
- Molecular Weight:332.87
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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κ Opioid Receptor/KOR |
μ Opioid Receptor/MOR |
Noribogaine hydrochloride (Increasing concentrations; 60 min at 25 °C) binds to human OPRK with higher affinity (Ki = 720 nM) than to human OPRM (Ki = 1520 nM) in competitive radioligand binding assays using CHO-K1 cell membranes[1].
Noribogaine hydrochloride (5-50 μM; 1-6 h) potently induces a dose-dependent increase in GDNF expression in SH-SY5Y human neuroblastoma cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y human neuroblastoma cells
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Concentration:5-50 μM
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Incubation Time:1 h; 3 h; 6 h
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Result:Induced a dose-dependent increase in GDNF expression similar to ibogaine, with a statistically significant effect for the 3-hour incubation.
Increased GDNF expression at 1 hour and 6 hours of incubation.
Noribogaine hydrochloride produces persistent inhibitory effects on the self-administration behaviors of various addictive agents in rats[1].
Noribogaine hydrochloride (40 mg/kg; i.p.; single administration) reaches high brain concentrations (~20 μM) after a single i.p. injection of 40 mg/kg Ibogaine in rats, exhibits excellent blood-brain barrier permeability, and induces centrally mediated prolactin release[1].
Noribogaine hydrochloride (1-100 μM; infused into the ventral tegmental area; administered for 2 minutes; 3 hours prior to the start of operant self-administration experiments) significantly, dose-dependently and persistently reduces operant ethanol self-administration behavior in rats with a history of high voluntary alcohol intake[2].
Noribogaine (20-40 mg/kg; i.p.; single administration) hydrochloride induces dose-dependent antidepressant-like effects in rats at 0.5 h after a single i.p. administration of 40 mg/kg, while no significant effects are observed at 3 h post-administration or in the 20 mg/kg dose group[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (adult male, 290-320 g for behavioral studies; 8-12 week old male, 280-300 g for pharmacokinetic studies)[1]
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Dosage:20 mg/kg; 40 mg/kg
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Administration:i.p.; single dose
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Result:Induced a significant decrease in immobility time and the 20 mg/kg dose at 0.5 hours post-40 mg/kg administration.
Showed no significant changes in swimming or climbing behavior at 0.5 hours post-administration.
Did not significantly alter locomotor activity in the open field test at 40 mg/kg dose.
Exhibited no significant effect on immobility time, swimming time, or climbing time at 3 hours post-administration.
Reached brain concentrations of 144 μM at 0.5 hours post-40 mg/kg dose and 31 μM at 3 hours post-40 mg/kg dose.
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Animal Model:Long-Evans rats with Alcohol use disorder (male, 280-300 g)[2]
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Dosage:0.8 μl of 1 μM (3 ng/μl); 0.8 μl of 10 μM (30 ng/μl); 0.8 μl of 100 μM (300 ng/μl)
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Administration:Intra-VTA infusion; over 2 minutes; 3 hours prior to operant self-administration sessions
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Result:Significantly reduced operant responding for ethanol.
Significantly reduced ethanol intake.
Produced a long-lasting decrease in ethanol deliveries that persisted for more than 48 hours post-infusion at 10 μM dose.
Produced a long-lasting decrease in ethanol intake that persisted for more than 48 hours post-infusion at 10 μM dose.
Exhibited similar long-lasting effects on ethanol deliveries and intake at 100 μM dose.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 110514-35-7
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Appearance Solid
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Molecular Weight 332.87
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Formula C19H25ClN2O
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Color Off-white to light yellow
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SMILES
CC[C@@H]1[C@@]2([H])[C@]3([H])C4=C(CC[N@]2C[C@@](C1)([H])C3)C5=CC(O)=CC=C5N4.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (281 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Maillet EL, et al. Noribogaine is a G-protein biased κ-opioid receptor agonist. Neuropharmacology. 2015;99:675-688. [Content Brief]
[2]. Carnicella S, et al. Noribogaine, but not 18-MC, exhibits similar actions as ibogaine on GDNF expression and ethanol self-administration. Addict Biol. 2010;15(4):424-433. [Content Brief]
[3]. Rodrı Guez P, et al. A Single Administration of the Atypical Psychedelic Ibogaine or Its Metabolite Noribogaine Induces an Antidepressant-Like Effect in Rats. ACS Chem Neurosci. 2020;11(11):1661-1672. [Content Brief]
[4]. Shi M, et al. A new approach methodology (NAM) for the prediction of (nor)ibogaine-induced cardiotoxicity in humans. ALTEX. 2021;38(4):636-652. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Noribogaine hydrochloride Related Classifications
HY-136832 Related Classifications
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