2. Neuronal Signaling GPCR/G Protein
  3. Serotonin Transporter Adrenergic Receptor 5-HT Receptor
  4. Z8779877149

Z8779877149 (Z7149) 是一种能够穿透血脑屏障的多靶点配体，靶向 SERT (Ki=198 nM)、α2A 肾上腺素能受体 (Ki=180 nM; EC50=440 nM) 及 5-HT2A 受体 (EC50=172 nM, Emax=76%)。Z8779877149 能通过抑制 5-HT 重摄取并分别激活 Gi 和 Gq 蛋白信号通路。Z8779877149 有效减轻了疼痛反应以及抑郁和焦虑样行为，同时展现出良好的安全性，不诱导镇静或运动障碍。Z8779877149 可研究疼痛、抑郁症及焦虑症。

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Z8779877149

Z8779877149 Chemical Structure

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Customer Review

Z8779877149 相关抗体

Top Publications Citing Use of Products

查看 Adrenergic Receptor 亚型特异性产品:

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α adrenergic receptor β adrenergic receptor

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

Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (Ki=198 nM), α2A adrenergic receptor (Ki=180 nM; EC50=440 nM) and 5-HT2A receptor (EC50=172 nM, Emax=76%). Z8779877149 inhibits 5-HT reuptake and activates Gi and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders[1].
IC50 & Target

α2-adrenergic receptor

180 nM (Ki)

5-HT2A Receptor

172 nM (EC50)

α2-adrenergic receptor

440 nM (EC50)

体外研究
(In Vitro)

Z8779877149 (z7149)(10-100 μM; 1 h) 可结合人源 α2A 肾上腺素受体和人源 SERT 的正构口袋，结合构象与对接预测基本一致，这一点已被冷冻电镜结构证实[1]。

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

Z8779877149 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Brain Concentration T1/2
Mice[1] 10 mg/kg i.p. 79.7 μM 830 nM 56 min
体内研究
(In Vivo)

Z8779877149 (腹腔注射，0.2-30 mg/kg) 可在急性、炎症性和神经性疼痛模型中产生依赖于 α2A 的镇痛作用，且无镇静效应或条件位置偏爱；在小鼠实验中，0.25 mg/kg 剂量下表现出类抗焦虑活性，0.5 mg/kg 剂量下表现出长效类抗抑郁活性[1]。

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

Animal Model: C57BL/6J (8-10 week-old male; 10-12 week-old male and female); α2A D79N mutant (7-8 week-old female); α2a knockout; VMAT2 heterozygous[1]
Dosage: 0.2 mg/kg (acute antidepressant-like activity); 0.25 mg/kg (anxiolytic-like activity); 0.5 mg/kg (antidepressant-like activity, acute and long-lasting); 10 mg/kg (analgesia, motor function, reward-related behavior); 20 mg/kg (analgesia); 30 mg/kg (analgesia)
Administration: i.p.
Result: Produced significant analgesia at 10 mg/kg; produced greater analgesic effects at 20 mg/kg and 30 mg/kg (increased withdrawal latency vs baseline).
Reduced CFA-induced thermal hypersensitivity at 10 mg/kg (significantly increased withdrawal latency vs vehicle-treated CFA mice).
Reduced SNI-induced mechanical allodynia at 10 mg/kg (significantly increased mechanical threshold vs vehicle-treated SNI mice).
Failed to produce significant analgesia at 10 mg/kg in α2A knockout mice.
Significantly increased punished crossings at 0.25 mg/kg, reaching an effect comparable to 0.5 mg/kg diazepam.
Reduced immobility time acutely at 0.2 mg/kg and 0.5 mg/kg with efficacy comparable to 20 mg/kg fluoxetine.
Maintained antidepressant-like efficacy for up to 5 days at 0.5 mg/kg, while fluoxetine efficacy declined by day 3.
Did not induce sedation or motor impairment at 10 mg/kg.
Did not induce conditioned place preference at 10 mg/kg.
分子量

326.31

Formula

C16H17F3N2O2
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

Z8779877149 相关分类

  • 摩尔计算器

  • 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.

Keywords:

Z8779877149Z7149Z 8779877149Z-8779877149Z 7149Z-7149Serotonin TransporterAdrenergic Receptor5-HT Receptor5-HTTSERTSLC6A4Beta ReceptorSerotonin Receptor5-hydroxytryptamine Receptordepressionanxiety5-HT2A receptorsGq protein signalingmouse modelsα2A adrenergic receptorsG? protein signalingpaincryo-EM structuresInhibitorinhibitorinhibit

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HY-181878
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