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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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κ Opioid Receptor/KOR |
μ Opioid Receptor/MOR |
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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.
Clinical Trial
| 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)
Protocols
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RT-PCR
Reverse transcription technology uses RNA as a template to synthesize DNA. RT-PCR is simple, specific and sensitive, and can be used to detect gene expression levels and expression differences in cells; detect RNA virus content; clone cDNA sequences of specific genes.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Real Time qPCR (Q-PCR)
Real-time quantitative PCR (qPCR) quantifies an amplifiable nucleic-acid target by monitoring fluorescence during PCR cycling rather than measuring product only after amplification. The increase in fluorescence tracks accumulation of PCR product, and the quantification cycle (Cq; historically also Ct/CP) is related to the initial amount of target: samples containing more starting target generally reach the defined fluorescence threshold in fewer cycles.
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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