Art. -Nr.: HY-106980

18-Methoxycoronaridine

Name: 18-Methoxycoronaridine
Brand: MedChemExpress
SKU: HY-106980
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(Synonyms: (-)-18-Methoxycoronaridine)

18-Methoxycoronaridine ((-)-18-Methoxycoronaridine) is an orally active and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist. 18-Methoxycoronaridine is an inhibitor of serotonin transporter (SERT) and norepinephrine transporter (NET), with IC₅₀ values of 51.6 μM and 121 μM for SERT and NET, respectively. 18-Methoxycoronaridine inhibits the function of SERT and NET, promotes 5-HT3A receptor desensitization, blocks α3β4 nAChR, and modulates receptor signaling pathways associated with reinforcement. 18-Methoxycoronaridine also exhibits potent antiparasitic activity. 18-Methoxycoronaridine can be used in research related to depression, obesity, alcoholism, smoking addiction, and cutaneous leishmaniasis.

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CAS. Nr.: 308123-60-6
Formel: C₂₂H₂₈N₂O₃
Molecular Weight:368.48

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

18-Methoxycoronaridine Chemical Structure

CAS. Nr.: 308123-60-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

Leishmania

5-HT_3A Receptor

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In Vitro

18-Methoxycoronaridine ((-)-18-Methoxycoronaridine) hydrochloride exhibits growth-inhibitory activity against intracellular amastigotes of Leishmania amazonensis^[5].
18-Methoxycoronaridine (0.3-300 μM; 60 min) hydrochloride binds to DAT, NET, and SERT in HEK293 cell membrane extracts with K_i values of 207 µM, 244 µM, and 12.6 µM, respectively^[2].
18-Methoxycoronaridine (0.3-300 μM; 10 min) hydrochloride inhibits substrate uptake by DAT, NET, and SERT in HEK293 cells with IC₅₀ values of 1177 µM, 121 µM, and 51.6 µM, respectively^[2].
18-Methoxycoronaridine (100 µM; 1-4 min) hydrochloride increases receptor desensitization in Xenopus oocytes expressing human 5-HT3A and 5-HT3AB receptors^[2].
18-Methoxycoronaridine (50 μM; 30 min) hydrochloride is metabolized to 18-hydroxycoronaridine (18-HC) in human liver microsomes and microsomes expressing CYP2C19^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

18-Methoxycoronaridine ((-)-18-Methoxycoronaridine) (20 mg/kg; p.o.; daily; for 5-10 consecutive days) hydrochloride significantly reduces tissue parasite burden in BALB/c mouse models infected with Leishmania amazonensis^[5].
18-Methoxycoronaridine (30-90 mg/kg; p.o.; once daily for 28 days) hydrochloride reduces lesion area and promotes healing in the Chlorocebus aethiops model infected with Leishmania amazonensis^[5].
18-Methoxycoronaridine (20-40 mg/kg; i.p.; single/daily administration; 14 consecutive days) hydrochloride induces antidepressant-like activity in male and female Swiss albino CD1 mice^[2].
18-Methoxycoronaridine (20 mg/kg; i.p.; single administration; observation for 24-72 h) hydrochloride reduces sucrose intake without inducing conditioned taste aversion in a female Sprague-Dawley rat model^[3].
18-Methoxycoronaridine (40 mg/kg; p.o.; single administration; 45 min) hydrochloride reduces nicotine self-administration behavior in female Sprague-Dawley rats^[4].
18-Methoxycoronaridine (10-40 mg/kg; p.o.; single administration; 6 h) hydrochloride dose-dependently reduces alcohol intake and preference in both male and female alcohol-preferring rat models^[4].
18-Methoxycoronaridine (10-30 mg/kg; i.p.; single administration; 240 min) hydrochloride reduces binge-like ethanol consumption in male and female C57BL/6J mouse models^[6].
18-Methoxycoronaridine (10-40 mg/kg; i.p.; single administration; 60 min) hydrochloride produces transient locomotor sedation in male C57BL/6J mice, while it has no effect on locomotor activity in female mice^[6].
18-Methoxycoronaridine (10-30 mg/kg; i.p.; single administration) hydrochloride has no effect on ethanol-induced sedation in the C57BL/6J mouse model^[6].
18-Methoxycoronaridine (20-30 mg/kg; i.p.; single administration; 180 min) hydrochloride has no effect on ethanol metabolism in the C57BL/6J mouse model^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Swiss albino CD1 (male and female, 30-35 g, forced swim test model)^[2]
Dosage:

40 mg/kg (acute treatment); 20 mg/kg (repeated treatment)
Administration:

i.p.; single dose (acute); once daily; 14 days (repeated)
Result:

Increased swimming time and decreased immobility time in both male and female mice at 1 h and 24 h post-acute 40 mg/kg injection, with no effect on climbing behavior.
Increased swimming time and decreased immobility time on day 7 and day 14 after repeated 20 mg/kg treatment, with no effect on climbing behavior.
Significantly reduced the increase in swimming time and reversed the decrease in immobility time induced by acute 40 mg/kg treatment following serotonin depletion pretreatment, with no alteration to lack of effect on climbing behavior.
Showed no change to swimming time, immobility time, or climbing behavior induced by acute 40 mg/kg treatment following norepinephrine depletion pretreatment.

Animal Model:

Swiss albino CD1 (male and female, 30-35 g, tail suspension test model)^[2]
Dosage:

40 mg/kg (acute treatment); 20 mg/kg (repeated treatment)
Administration:

i.p.; single dose (acute); once daily; 14 days (repeated)
Result:

Reduced immobility time in both male and female mice at 24 h post-acute 40 mg/kg injection, with no effect on lateral swing or running behaviors.
Reduced immobility time on day 7 and day 14 after repeated 20 mg/kg treatment, with no effect on lateral swing behavior.

Animal Model:

Sprague-Dawley (female, 230-270 g)^[3]
Dosage:

20 mg/kg
Administration:

i.p.; single injection; 24, 48, 72 h
Result:

Reduced sucrose intake 24 hours post-treatment when injected immediately after 15 minutes of sucrose access.
Reduced sucrose intake by 54% at 24 hours and 28% at 48 hours post-treatment when injected 1 hour after a 30-minute sucrose access session.
Showed no effect on sucrose intake at 72 hours post-treatment when injected 1 hour after a 30-minute sucrose access session.
Showed no effect on sucrose intake at 72 hours post-treatment when injected immediately after 15 minutes of sucrose access.
Left water intake unchanged in all experiments.

Animal Model:

Sprague-Dawley (young adult female, 150-250 g, nicotine self-administration model)^[4]
Dosage:

40 mg/kg
Administration:

p.o.; single dose; 45 min
Result:

Reduce nicotine self-administration behavior in female Sprague-Dawley rats.

Animal Model:

Alcohol-preferring (P) (adult male and female, alcohol intake model)^[4]
Dosage:

10 mg/kg; 20 mg/kg; 40 mg/kg
Administration:

p.o.; single dose; 6 h
Result:

Decreased alcohol consumption (g/kg) over 6 hours at all doses.
Decreased alcohol preference relative to water at 20 mg/kg and 40 mg/kg.
Did not significantly affect water intake.
Showed no significant differences in efficacy between male and female rats.

Animal Model:

C57BL/6J (adult male and female, 5-6 weeks of age at arrival, binge-like ethanol consumption induced via Drinking-in-the-Dark paradigm)^[6]
Dosage:

10 mg/kg; 20 mg/kg; 30 mg/kg
Administration:

i.p.; single injection; 30, 60, 120, 240 min
Result:

Decreased ethanol consumption compared to saline-treated mice at 60, 120, and 240 minutes at 30 mg/kg.
Decreased ethanol consumption compared to the 10 mg/kg dose at 120 minutes at 30 mg/kg.
Did not significantly alter saccharin consumption at any tested dose.
Showed no sex interaction with efficacy, though female mice consumed significantly more ethanol than males at 240 minutes.

Animal Model:

C57BL/6J (adult male and female, 5-6 weeks of age at arrival, locomotor activity assessment)^[6]
Dosage:

10 mg/kg; 20 mg/kg; 30 mg/kg; 40 mg/kg
Administration:

i.p.; single injection; 60 min
Result:

Reduced locomotor activity at 20, 30, and 50 minutes in male mice at 30 mg/kg.
Reduced locomotor activity at 20, 30, 40, and 50 minutes in male mice at 40 mg/kg.
Did not significantly alter male locomotor activity at 20 mg/kg.
Produced no significant effects on locomotor activity in female mice at any tested dose.

Animal Model:

C57BL/6J (adult male and female, 5-6 weeks of age at arrival, ethanol metabolism assessment)^[6]
Dosage:

20 mg/kg; 30 mg/kg
Administration:

i.p.; single injection; 30, 60, 180 min
Result:

Did not produce significant differences in blood ethanol concentrations at any tested time point or dose in male or female mice.
Showed higher blood ethanol concentrations at 30 and 60 minutes compared to 180 minutes in male mice in saline and 20 mg/kg groups.
Showed higher blood ethanol concentrations at 60 minutes compared to 180 minutes in male mice at 30 mg/kg.
Showed time-dependent decrease in blood ethanol concentrations across all groups in female mice.

Animal Model:

BALB/c (male and female, 4 weeks old, 20-25 g, infected with Leishmania amazonensis promastigotes 30 days prior to treatment)^[5]
Dosage:

20 mg/kg
Administration:

p.o.; once daily; 5, 10 consecutive days
Result:

Reduced parasite burden by 99.9% in infected paws and 99.9% in popliteal lymph nodes after 5 days of treatment compared to untreated controls.
Reduced parasite burden by 99.98% in infected paws after 10 days of treatment compared to untreated controls.

Animal Model:

Chlorocebus aethiops (male and female, 1.5-3 years old, inoculated with Leishmania amazonensis promastigotes 30 days prior to treatment)^[5]
Dosage:

30 mg/kg; 90 mg/kg
Administration:

p.o.; once daily; 28 consecutive days
Result:

Reduced lesion area by 67% at 2 months post-infection with 30 mg/kg/day treatment compared to controls.
Reduced lesion area by 98% at 2 months post-infection with 90 mg/kg/day treatment compared to controls.
Achieved 80% healed lesions in the 30 mg/kg/day group compared to controls.
Achieved 80% healed lesions with 20% showing late-stage lesion regression in the 90 mg/kg/day group compared to controls.
Demonstrated an exposure-dependent efficacy response with an EC₅₀ of 209 ng·h/mL and an index of approximately 5.4.

Related Protocols :

Research Protocol for Metabolic Diseases

Chemical Information

CAS. Nr. 308123-60-6
Molecular Weight 368.48
Formel C₂₂H₂₈N₂O₃
SMILES

C(OC)(=O)[C@]12[C@]3([N@](C[C@@](C1)(C[C@@H]3CCOC)[H])CCC4=C2NC=5C4=CC=CC5)[H]
Synonyms

(-)-18-Methoxycoronaridine
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Zhang W, et al. Metabolism of 18-methoxycoronaridine, an ibogaine analog, to 18-hydroxycoronaridine by genetically variable CYP2C19. Drug metabolism and disposition: the biological fate of chemicals. 2002 Jun;30(6):663-9.

[2]. Arias HR, et al. (+)-Catharanthine and (-)-18-methoxycoronaridine induce antidepressant-like activity in mice by differently recruiting serotonergic and norepinephrinergic neurotransmission. European journal of pharmacology. 2023 Jan 15;939:175454. [Content Brief]

[3]. Taraschenko OD, et al. 18-Methoxycoronaridine, a potential anti-obesity agent, does not produce a conditioned taste aversion in rats. Pharmacology, biochemistry, and behavior. 2010 Sep;96(3):247-50.

[4]. Rezvani AH, et al. Acute oral 18-methoxycoronaridine (18-MC) decreases both alcohol intake and IV nicotine self-administration in rats. Pharmacology, biochemistry, and behavior. 2016;150-151:153-157.

[5]. Delorenzi JC, et al. Oral 18-methoxycoronaridine activity in simian and murine Leishmania amazonensis infection. Front Pharmacol. 2026 Apr 10;17:1780255. [Content Brief]

[6]. Miller CN, et al. The α3β4 nicotinic acetylcholine receptor antagonist 18-Methoxycoronaridine decreases binge-like ethanol consumption in adult C57BL/6J mice. Alcohol. 2019 Sep;79:1-6. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

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18-Methoxycoronaridine

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