2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 5-HT2A&5-HT2C agonist-3

5-HT2A&5-HT2C agonist-3 (compound 4e) 是一种具有口服生物利用度和血脑屏障穿透性的 5-HT2A 和 5-HT2C 激动剂。5-HT2A&5-HT2C agonist-3 可使过表达 5-HT2A 或 5-HT2C 受体的细胞内钙水平升高，且对 5-HT2B 受体无活性。5-HT2A&5-HT2C agonist-3 可用于神经精神疾病的研究。

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5-HT2A&5-HT2C agonist-3

5-HT2A&5-HT2C agonist-3 Chemical Structure

CAS No. : 3082429-35-1

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5-HT2A&5-HT2C agonist-3 相关抗体

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查看 5-HT Receptor 亚型特异性产品:

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

5-HT2A&5-HT2C agonist-3 (compound 4e) is an orally bioavailable and blood-brain barrier penetrant agonist of 5-HT2A and 5-HT2C. 5-HT2A&5-HT2C agonist-3 increases intracellular calcium levels in cells overexpressing 5-HT2A or 5-HT2C receptors, and shows no activity against 5-HT2B receptors. 5-HT2A&5-HT2C agonist-3 can be used for the research of neuropsychiatric disorders[1].

体外研究
(In Vitro)

5-HT2A&5-HT2C agonist-3 (compound 4e) 是 CHO-K1 细胞中表达的人源 5-HT2A 和 5-HT2C 受体的选择性部分激动剂，对 5-HT2B 受体无可检测的效能，在 5-HT2A 受体上的 pEC50 为 7.79，在 5-HT2C 受体上的 pEC50 为 7.10[1]。

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

5-HT2A&5-HT2C agonist-3 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route AUC Cmax Tmax
Mice[1] 20 mg/kg p.o. 8903 ng·h/mL 5426 ng/mL 0.25 h
体内研究
(In Vivo)

5-HT2A&5-HT2C agonist-3 (compound 4e) (3 mg/kg; p.o.; single dose) 相较于等剂量 (3 mg/kg 口服) 的裸盖菇素，可显著减弱雄性 C57BL/6 小鼠类迷幻药的甩头反应[1]。

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

Animal Model: C57BL/6 (male)[1]
Dosage: 3 mg/kg
Administration: p.o.; single dose
Result: Induced a significantly lower total number of head-twitch responses compared to both 1 mg/kg and 3 mg/kg doses of psilocybin.
Did not elicit an early peak response; instead, showed a delayed and attenuated profile, with a modest increase in head-twitch responses observed primarily in intermediate and later 10-minute intervals of the 45-minute observation period.
分子量

365.78

Formula

C15H19ClF3N3O2
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

5-HT2A&5-HT2C agonist-3 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

5-HT2A&5-HT2C agonist-33082429-35-15-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorS9 fractionshuman plasmaCHO-K1 cellsmale C57BL/6 mice5-HT2C receptorshuman liver microsomes5-HT2B receptors5-HT2A receptorsneuropsychiatric conditionspsilocinInhibitorinhibitorinhibit

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