Milnacipran

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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 (K_i 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).

For research use only. We do not sell to patients.

Milnacipran Chemical Structure

CAS No. : 92623-85-3

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5 mg	Get quote	Estimated Time of Arrival: December 31
10 mg	Get quote	Estimated Time of Arrival: December 31
25 mg	Get quote	Estimated Time of Arrival: December 31

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Other Forms of Milnacipran:

2 Publications Citing Use of MCE Milnacipran

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Biological Activity
Purity & Documentation
References
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Description

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]

In Vitro

Milnacipran shows high affinity for 5-HT and NA transporters (K_i = 8.5 and 31 nM, respectively)^[2].
Milnacipran (10-100 µM; 3 min) reduces the amplitude of NMDA (HY-17551)-induced currents in rat spinal lamina II neurons^[5].
Milnacipran (100 µM; 10 min) suppresses NMDA (HY-17551)-induced pERK1/2 activation in superficial dorsal horn neurons^[5].

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

In Vivo

Milnacipran (30-60 mg/kg; p.o.; single dose) shows anxiolytic effects in rats^[2].
Milnacipran (30-120 mg/kg; p.o.) increases withdrawal threshold to tactile stimulation and latency to heat stimulation in a dose-dependent manner in rats with spinal nerve ligation (SNL)^[4].
Milnacipran (0.01-0.1 µmol; intrathecal) suppresses hyperalgesia in a dose-dependent manner in mice with intrathecal NMDA-induced thermal hyperalgesia^[5].
Milnacipran (3-30 mg/kg; i.p.) suppresses impulsive, aggressive, and depressive-like behaviors in male C57BL/6N mice^[6].
Milnacipran (20-60 mg/kg; i.p.) suppresses food intake in fasted male C57BL/6J and A^y mice, increases hypothalamic POMC and CART mRNA levels, and does not elevate plasma corticosterone or blood glucose^[7].
Milnacipran (0.1-10 μg/site; intrathecal) inhibits Serotonin-induced biting behavior in male ICR mice^[8].

MedChemExpress (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

Molecular Weight

246.35

Formula

C₁₅H₂₂N₂O

CAS No.

92623-85-3

SMILES

CCN(CC)C([C@@]1(C2=CC=CC=C2)[C@H](C1)CN)=O

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

Handling Instructions (2659 KB)

References

[1]. Chen C, et al. Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9. [Content Brief]

[2]. Mochizuki D, et al. Neurochemical and behavioural characterization of milnacipran, a serotonin and noradrenaline reuptake inhibitor in rats. Psychopharmacology (Berl). 2002 Jul;162(3):323-32. [Content Brief]

[3]. Ueta K, et al. In vitro inhibition of recombinant ligand-gated ion channels by high concentrations of milnacipran. Psychopharmacology (Berl). 2004 Sep;175(2):241-6. [Content Brief]

[4]. Suzuki T, et al. Antiallodynic and antihyperalgesic effect of milnacipran in mice with spinal nerve ligation. Anesth Analg. 2008 Apr;106(4):1309-15, table of contents. [Content Brief]

[5]. Kohno T, et al. Milnacipran inhibits glutamatergic N-methyl-D-aspartate receptor activity in spinal dorsal horn neurons. Mol Pain. 2012 Jun 19;8:45. [Content Brief]

[6]. Tsutsui-Kimura I, et al. Milnacipran affects mouse impulsive, aggressive, and depressive-like behaviors in a distinct dose-dependent manner. J Pharmacol Sci. 2017 Jul;134(3):181-189. [Content Brief]

[7]. Nonogaki K, et al. Milnacipran, a serotonin and norepinephrine reuptake inhibitor, induces appetite-suppressing effects without inducing hypothalamic stress responses in mice. Am J Physiol Regul Integr Comp Physiol. 2007 May;292(5):R1775-81. [Content Brief]

[8]. Andoh T, et al. Milnacipran inhibits itch-related responses in mice through the enhancement of noradrenergic transmission in the spinal cord. J Pharmacol Sci. 2013;123(2):199-202. [Content Brief]

Milnacipran Related Classifications

Neurological Disease

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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:

Milnacipran92623-85-3Serotonin TransporterPERK5-HTTSERTSLC6A4Protein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasemicethermal hyperalgesiaantidepressantanxiolytic and analgesicsuperficial dorsal horn neuronsRatInhibitorinhibitorinhibit

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