2. GPCR/G Protein Neuronal Signaling Others
  3. 5-HT Receptor Drug Derivative
  4. 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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R-MDDMA

R-MDDMA Chemical Structure

CAS No. : 872679-98-6

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R-MDDMA Related Antibodies

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Description

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[1].

IC50 & Target[1]

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)

In Vitro

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.

R-MDDMA Related Antibodies

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-MDDMA (12.5-50 mg/kg; i.p.; single dose) does not induce hyperthermia, hyperlocomotion, or head-twitch responses at 12.5 mg/kg, 25 mg/kg, though the 50 mg/kg dose causes transient hypothermia, reduced locomotion, and increased thigmotaxis[1].
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.

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: 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.
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: 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).
Molecular Weight

206.28

Formula

C13H18O2
CAS No.
SMILES

C[C@H](CC1=CC2=C(C=C1)OCO2)C(C)C
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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R-MDDMA Related Classifications

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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.

Keywords:

R-MDDMA872679-98-65-HT ReceptorDrug DerivativeSerotonin Receptor5-hydroxytryptamine ReceptorDrug derivative5-HT2C receptorcortical neuronsmouse cued fear conditioning modelpreclinical rodent models5-HT2A receptorpost-traumatic stress disorderdepression5-HT2B receptorGq signalingHEK293T cellsInhibitorinhibitorinhibit

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