Formulation: A solid
Formal Name: (1R,2S)-2-(aminomethyl)-N,N-diethyl-1-(phenyl-d5)cyclopropane-1-carboxamide, monohydrochloride
Purity: ≥99% deuterated forms (d1-d5)
Formula Markup: C15H17D5N2O • HCl
Formula Weight: 287,8
Shelf life (days): 1460
Notes: Milnacipran-d5 is intended for use as an internal standard for the quantification of milnacipran (Item No. 23837) by GC- or LC-MS. 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, 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 in the treatment of fibromyalgia pain.