A serotonin and norepinephrine reuptake inhibitor; selectively inhibits the human serotonin transporter and norepinephrine transporter over the dopamine transporter (IC50s = 420

Milnacipran (hydrochloride) – 250 mg

Brand:
Cayman
CAS:
101152-94-7
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Milnacipran is an orally bioavailable serotonin and norepinephrine reuptake inhibitor (SNRI).{41447} It selectively inhibits the human serotonin transporter and norepinephrine transporter over the dopamine transporter (IC50s = 420, 77, and 6,100 nM, respectively). It also selectively inhibits sodium-dependent serotonin (Item No. 14332) and norepinephrine (Item No. 16673) uptake over dopamine (Item No. 21992) uptake in rat cerebral cortical synaptosomes (IC50s = 28.0, 29.6, and >10,000 nM, respectively).{41448} Milnacipran is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3A as well as nicotinic acetylcholine receptors (nAChRs; IC50s = 63.5 and 14.3 μM, respectively) but does not inhibit other 5-HT, adrenergic, dopamine, muscarinic acetylcholine (mACh), histamine, NMDA, sigma, opioid, or GABA receptors (Kis = >10,000 nM).{41448,41449} In vivo, milnacipran (30 mg/kg) increases withdrawal threshold and latency in response to tactile and heat stimulation, respectively, in nerve-ligated mice.{41450} Formulations containing milnacipran have been used to treat fibromyalgia pain.  

 

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Description

A serotonin and norepinephrine reuptake inhibitor; selectively inhibits the human serotonin transporter and norepinephrine transporter over the dopamine transporter (IC50s = 420, 77, and 6,100 nM, respectively); inhibits sodium-dependent serotonin and norepinephrine uptake over dopamine uptake in rat cerebral cortical synaptosomes (IC50s = 28.0, 29.6, and >10,000 nM, respectively); is an antagonist of the 5-HT3A and nAChRs (IC50s = 63.5 and 14.3 μM, respectively); increases withdrawal threshold and latency in response to tactile and heat stimulation, respectively, in nerve-ligated mice (30 mg/kg)

Formal name: (1R,2S)-rel-2-(aminomethyl)-N,N-diethyl-1-phenyl-cyclopropanecarboxamide, monohydrochloride

Synonyms:  F 2207

Molecular weight: 282.8

CAS: 101152-94-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Neuroscience|Pain Research

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