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

R-MDDMA,一种亚甲二氧基甲基苯丙胺 (MDMA) 类似物,是 5-HT2A/5-HT2C 受体调节剂。R-MDDMA 对 5-HT2A/5-HT2C 具有拮抗活性,其 IC50 值分别为 642 和 137 nM,同时还具有部分激动剂活性,EC50 值分别为 24.5 和 14.4 nM,但不会激活 5-HT2B 受体。R-MDDMA 可促进皮质神经元生长。R-MDDMA 可促进恐惧消退学习,并在临床前啮齿动物模型中产生类抗抑郁作用。R-MDDMA 可用于创伤后应激障碍和抑郁症的研究。

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R-MDDMA

R-MDDMA Chemical Structure

CAS No. : 872679-98-6

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Other Forms of R-MDDMA:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

R-MDDMA (10 pM-10 μM; 24-72 h) 可强效通过 5-HT2 受体依赖机制促进 E18 胚胎大鼠皮层神经元的生长[1]
R-MDDMA (100 μM; 15 min) 不会诱导表达 SERT 的 HEK293T 细胞发生血清素外流[1]
R-MDDMA (10 pM-100 μM; 5 min) 在表达 psychLight2 生物传感器的 HEK293T 细胞中作为中等效力的 5-HT2A 受体拮抗剂,其 IC50 为 642 nM[1]
R-MDDMA (10 pM-100 μM; 5 min) 在表达 GRAB5-HT 生物传感器的 HEK293T 细胞中作为 5-HT2C 受体的强效拮抗剂,其 IC50 为 137 nM[1]
R-MDDMA (1 pM-1000 μM; 5 min) 是 5-HT2A 和 5-HT2C 受体的部分激动剂 (EC50 = 24.5 nM 和 14.4 nM),但在 HEK293T 细胞中不会激活 5-HT2B 受体[1]

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.
体内研究
(In Vivo)

R-MDDMA (12.5-50 mg/kg;腹腔注射;单次给药) 在治疗相关剂量 (12.5 mg/kg, 25 mg/kg) 下不会诱导体温过高、运动过度或甩头反应,但 50 mg/kg 剂量会引起短暂性体温过低、运动减少及趋触性增加[1]
R-MDDMA (12.5-25 mg/kg;腹腔注射;单次给药;消退训练前 30 min) 在小鼠线索性恐惧条件化模型中,可促进持续性恐惧消退学习[1]
R-MDDMA (12.5-25 mg/kg;腹腔注射;单次给药) 在小鼠悬尾实验中产生持续的类抗抑郁作用[1]
R-MDDMA (12.5-25 mg/kg;腹腔注射;单次给药) 对小鼠三室社交互动实验或社交条件性位置偏爱实验未产生具有统计学意义的亲社会效应[1]

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).
分子量

206.28

Formula

C13H18O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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-MDDMA
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HY-186169
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