1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. R-MDMA

R-MDMA, 4-methylenedioxymethamphetamine (MDMA) isomer, is a 5-HT2A/5-HT2C receptor antagonist with an IC50 of 629 and 61.4 nM. R-MDMA promotes cortical neuron growth. R-MDMA facilitates fear extinction learning and produces antidepressant-like effects in preclinical rodent models. R-MDMA can be used for the researches of post-traumatic stress disorder and depression.

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R-MDMA

R-MDMA Chemical Structure

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Description

R-MDMA, 4-methylenedioxymethamphetamine (MDMA) isomer, is a 5-HT2A/5-HT2C receptor antagonist with an IC50 of 629 and 61.4 nM. R-MDMA promotes cortical neuron growth. R-MDMA facilitates fear extinction learning and produces antidepressant-like effects in preclinical rodent models. R-MDMA can be used for the researches of post-traumatic stress disorder and depression[1].

IC50 & Target[1]

5-HT2C Receptor

61.4 nM (IC50)

5-HT2A Receptor

629 nM (IC50)

In Vitro

R-MDMA (10 pM-10 μM; 24-72 h) promotes cortical neuron growth[1].

R-MDMA (100 μM; 15 min) induces serotonin efflux from SERT-expressing HEK293T cells[1].
R-MDMA (10 pM-100 μM; 5 min) acts as a moderately potent antagonist at 5-HT2A receptors in HEK293T cells with an IC50 of 629 nM[1].
R-MDMA (10 pM-100 μM; 5 min) acts as a moderately potent antagonist at 5-HT2C receptors in HEK293T cells with an IC50 of 61.4 nM[1].

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

Cell Proliferation Assay[1]

Cell Line: cortical neurons
Concentration: 10 pM, 1, 100 nM, 10 μM
Incubation Time: 24, 72 h
Result: Promoted cortical neuron growth.
In Vivo

R-MDMA (12.5-50 mg/kg; i.p.; single dose) decreases locomotion at 12.5 mg/kg, increases locomotion at 50 mg/kg, increases thigmotaxis at all tested doses, causes transient body temperature decreases at 25 mg/kg and 50 mg/kg, and does not induce head-twitch responses at any tested dose[1].
R-MDMA (12.5-25 mg/kg; i.p.; single dose; 30 min prior to extinction training) facilitates fear extinction learning, producing sustained reductions in freezing behavior in a mouse fear conditioning model[1].
R-MDMA (12.5-25 mg/kg; i.p.; single dose) at 25 mg/kg produces a sustained antidepressant-like effect in the mouse tail suspension test[1].
R-MDMA (20 mg/kg; i.p.; single dose; administered during social interaction training sessions) does not produce a statistically significant social conditioned place preference in mice[1].

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

Animal Model: C57BL/6J (9-13 weeks old, mixed male and female)[1]
Dosage: 12.5 mg/kg; 25 mg/kg; 50 mg/kg
Administration: i.p.; single dose
Result: Decreased locomotion at 12.5 mg/kg.
Increased locomotion at 50 mg/kg.
Caused significantly less time spent in the arena center (increased thigmotaxis) at all doses.
Did not induce head-twitch response at any dose.
Caused transient decrease in body temperature at 30 min post-administration of 25 mg/kg and 50 mg/kg, which resolved by 60 min.
Produced no body temperature changes at 12.5 mg/kg.
Animal Model: Depressant C57BL/6J (9-13 weeks old, mixed male and female)[1]
Dosage: 12.5 mg/kg; 25 mg/kg
Administration: i.p.; single dose
Result: Reduced immobility time to a comparable extent to positive control Ketamine (3 mg/kg) at 25 mg/kg.
Did not produce statistically significant antidepressant-like response at 12.5 mg/kg.
Had its antidepressant-like effect blocked when pretreated with 5-HT2 antagonist Ketanserin (HY-10562) (4 mg/kg, i.p., 10 min prior) at 25 mg/kg.
Molecular Weight

192.25

Formula

C12H16O2

SMILES

C[C@@H](CC1=CC2=C(C=C1)OCO2)CC

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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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.

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R-MDMA
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HY-186170
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