2. Neuronal Signaling Cell Cycle/DNA Damage
  3. Serotonin Transporter PERK
  4. Milnacipran

Milnacipran 是一种口服活性的 Serotonin (HY-B1473A) 和 Norepinephrine (HY-13715) 再摄取抑制剂。Milnacipran 抑制单胺转运体 (尤其是去甲肾上腺素转运体和 5-羟色胺转运体 (Ki 值分别为 31 和 8.5 nM))。Milnacipran hydrochloride 抑制 pERK1/2 激活。Milnacipran 具有抗抑郁、抗焦虑和镇痛作用。Milnacipran 抑制小鼠咬合行为。Milnacipran 可用于重度抑郁症、焦虑症、神经性疼痛 (如纤维肌痛) 研究。

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Milnacipran

Milnacipran Chemical Structure

CAS No. : 92623-85-3

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Other Forms of Milnacipran:

Milnacipran 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Milnacipran is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran inhibits pERK1/2 activation. Milnacipran has antidepressant, anxiolytic and analgesic properties. Milnacipran inhibits biting behavior in mice. Milnacipran can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia)[1][2][3][4][5][6][7][8].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
64 nM
Compound: rel-Milnacipran
Inhibition of human SERT expressed in CHO cell membranes assessed as reduction in [3H]serotonin uptake preincubated for 10 mins followed by [3H]serotonin addition measured after 20 mins by liquid scintillation counting method
Inhibition of human SERT expressed in CHO cell membranes assessed as reduction in [3H]serotonin uptake preincubated for 10 mins followed by [3H]serotonin addition measured after 20 mins by liquid scintillation counting method
[PMID: 27865645]
体外研究
(In Vitro)

Milnacipran 对 5-HT 和 NA 转运体具有高亲和力 (Ki 分别为 8.5 和 31 nM)[2]。
Milnacipran (10-100 µM；3 min) 可降低大鼠脊髓 II 层神经元中 NMDA (HY-17551) 诱导电流的幅度[5]。
Milnacipran (100 µM；10 min) 可抑制浅表背角神经元中 NMDA (HY-17551) 诱导的 pERK1/2 激活[5]。

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

Milnacipran 相关抗体:
体内研究
(In Vivo)

Milnacipran (30-60 mg/kg；口服；单剂量) 对大鼠有抗焦虑作用[2]。
Milnacipran (30-120 mg/kg；口服) 以剂量依赖性方式增加脊髓神经结扎 (SNL) 大鼠对触觉刺激的戒断阈值和对热刺激的潜伏期[4]。
Milnacipran (0.01-0.1 µmol；鞘内注射) 以剂量依赖性方式抑制鞘内 NMDA 诱发的热痛觉过敏小鼠的痛觉过敏[5]。
Milnacipran (3-30 mg/kg；腹腔注射) 可抑制雄性 C57BL/6N 小鼠的冲动、攻击和抑郁样行为小鼠[6]。
Milnacipran (20-60 mg/kg；腹腔注射) 可抑制禁食雄性 C57BL/6J 和 Ay 小鼠的食物摄入，提高下丘脑 POMC 和 CART mRNA 水平，并且不会升高血浆皮质酮或血糖[7]。
Milnacipran (0.1-10 μg/部位；鞘内注射) 可抑制雄性 ICR 小鼠血清素诱导的咬合行为[8]。

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

Animal Model: Male Sprague-Dawley rats; conditioned fear stress test[2]
Dosage: 10, 30, 60 mg/kg
Administration: Oral administration (p.o.), single dose 60 min before testing.
Result: Reduced freezing time at 30 and 60 mg/kg.
Animal Model: Male C57BL/6N mice and male BALB/c mice[6]
Dosage: 0, 3, 10, 30 mg/kg (saline)
Administration: Intraperitoneal injection (i.p.); 60 min prior to each test; single dose per session with washout intervals (1 week for 3-CSRTT, 2 days for RIT).
Result: Reduced premature responses in 3-CSRTT and attack bites in RIT, shortened immobility time in FST (at 10 mg/kg).
Increased aggressive behavior and elevated dopamine levels in the nucleus accumbens (at 30 mg/kg).
Clinical Trial
分子量

246.35

Formula

C15H22N2O
CAS 号
中文名称

米那普仑杂质1
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

Milnacipran 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:

Milnacipran92623-85-3米那普仑杂质1Serotonin TransporterPERK5-HTTSERTSLC6A4Protein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasemicethermal hyperalgesiaantidepressantanxiolytic and analgesicsuperficial dorsal horn neuronsRatInhibitorinhibitorinhibit

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