2. Neuronal Signaling Membrane Transporter/Ion Channel GPCR/G Protein
  3. Serotonin Transporter Potassium Channel Arrestin Opioid Receptor
  4. Noribogaine hydrochloride

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.

Noribogaine hydrochloride

Noribogaine hydrochloride Chemical Structure

CAS No. : 110514-35-7

Size Price Stock Quantity
500 μg In-stock
1 mg In-stock
5 mg   Get quote  
10 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Noribogaine hydrochloride Related Antibodies

Top Publications Citing Use of Products

View All Arrestin Isoform Specific Products:

View All Isoforms
Arrestin-2/β-Arrestin 1 Arrestin-3/β-Arrestin 2

View All Opioid Receptor Isoform Specific Products:

View All Isoforms
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4].

IC50 & Target

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.

Noribogaine hydrochloride Related Antibodies

RT-PCR[2]

Cell Line: SH-SY5Y human neuroblastoma cells
Concentration: 5-50 μM
Incubation Time: 1 h; 3 h; 6 h
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 (10-40 mg/kg; i.p.) restores the anti-nociceptive activity of morphine in morphine-tolerant mice at doses of 10 and 20 mg/kg, enhances morphine-induced analgesic effects at a dose of 40 mg/kg, and prevents the development of morphine analgesic tolerance[1].
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.

Animal Model: Wistar rats (adult male, 290-320 g for behavioral studies; 8-12 week old male, 280-300 g for pharmacokinetic studies)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: i.p.; single dose
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.
Animal Model: Long-Evans rats with Alcohol use disorder (male, 280-300 g)[2]
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)
Administration: Intra-VTA infusion; over 2 minutes; 3 hours prior to operant self-administration sessions
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
Molecular Weight

332.87

Formula

C19H25ClN2O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
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

Purity: 99.9%

SDS (394 KB)

COA (253 KB) MS (193 KB)

Handling Instructions (2659 KB)
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Noribogaine hydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

Noribogaine110514-35-7Serotonin TransporterPotassium ChannelArrestinOpioid Receptor5-HTTSERTSLC6A4KcsAOPRMhERG channelhiPSC-CMsOPRKCaco-2 cellshuman liver microsomesCHO-K1 cellsratsSH-SY5Y human neuroblastoma cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Noribogaine hydrochloride
Cat. No.:
HY-136832
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.