R-MDDMA
R-MDDMA, 4-methylenedioxymethamphetamine (MDMA) analogue, is a 5-HT2A/5-HT2C receptor modulator. R-MDDMA shows antagonistic activity against 5-HT2A/5-HT2C with IC50 values of 642 and 137 nM, and also shows partial agonist activity with EC50 values of 24.5 and 14.4 nM, but does not activate 5-HT2B receptors. R-MDDMA promotes cortical neuron growth. R-MDDMA facilitates fear extinction learning and produces antidepressant-like effects in preclinical rodent models. R-MDDMA can be used for the researches of post-traumatic stress disorder and depression.
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- CAS No.: 872679-98-6
- Formule: C13H18O2
- Masse moléculaire:206.28
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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5-HT2C Receptor 137 nM (IC50) |
5-HT2A Receptor 642 nM (IC50) |
5-HT2C Receptor 14.4 nM (EC50) |
5-HT2A Receptor 24.5 nM (EC50) |
R-MDDMA (10 pM-10 μM; 24-72 h) potently promotes growth of E18 embryonic rat cortical neurons via a 5-HT2 receptor-dependent mechanism[1].
R-MDDMA (100 μM; 15 min) does not induce serotonin efflux from SERT-expressing HEK293T cells[1].
R-MDDMA (10 pM-100 μM; 5 min) acts as a moderately potent antagonist at 5-HT2A receptors in HEK293T cells expressing the psychLight2 biosensor, with an IC50 of 642 nM[1].
R-MDDMA (10 pM-100 μM; 5 min) acts as a potent antagonist at 5-HT2C receptors in HEK293T cells expressing the GRAB5-HT biosensor, with an IC50 of 137 nM[1].
R-MDDMA (1 pM-1000 μM; 5 min) acts as a partial agonist of 5-HT2A and 5-HT2C receptors (EC50 = 24.5 nM and 14.4 nM, respectively) but does not activate 5-HT2B receptors in HEK293T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:cortical neurons
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Concentration:10 pM, 1, 100 nM, 10 μM
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Incubation Time:24, 72 h
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Result:Promoted cortical neuron growth.
R-MDDMA (12.5-25 mg/kg; i.p.; single dose; 30 min prior to extinction training) facilitates sustained fear extinction learning in a mouse cued fear conditioning model[1].
R-MDDMA (12.5-25 mg/kg; i.p.; single dose) produces a sustained antidepressant-like effect in the mouse tail suspension test[1].
R-MDDMA (12.5-25 mg/kg; i.p.; single dose) does not produce statistically significant prosocial effects in mouse 3-chamber social interaction or social conditioned place preference assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (9−13 weeks old, mixed male and female)[1]
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Dosage:12.5 mg/kg; 25 mg/kg; 50 mg/kg
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Administration:i.p.; single dose
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Result:Did not produce statistically significant changes in locomotion or thigmotaxis at 12.5 mg/kg and 25 mg/kg.
Decreased locomotion and increased thigmotaxis at 50 mg/kg.
Did not induce head-twitch response at any dose.
Caused transient decrease in body temperature at 30 min post-administration with 50 mg/kg dose, which resolved within 30 min.
Did not detect body temperature changes with 12.5 mg/kg or 25 mg/kg doses over 2 hours.
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Animal Model:Depressant C57BL/6J (9-13 weeks old, mixed male and female)[1]
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Dosage:12.5 mg/kg; 25 mg/kg
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Administration:i.p.; single dose
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Result:Did not reduce immobility time in the tail suspension test at 12.5 mg/kg dose.
Reduced immobility time to a comparable extent as positive control ketamine (3 mg/kg) at 25 mg/kg dose.
Completely blocked antidepressant-like effect of 25 mg/kg dose by pretreatment with 5-HT2 antagonist Ketanserin (HY-10562).
Chemical Information
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CAS No. 872679-98-6
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Masse moléculaire 206.28
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Formule C13H18O2
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SMILES
C[C@H](CC1=CC2=C(C=C1)OCO2)C(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
R-MDDMA Related Classifications
HY-186169 Related Classifications
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