Milnacipran (hydrochloride)

Milnacipran is an orally bioavailable serotonin and norepinephrine reuptake inhibitor (SNRI). 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 (Cay-14332) and norepinephrine (Cay-16673) uptake over dopamine (Cay-21992) uptake in rat cerebral cortical synaptosomes (IC50s = 28.0, 29.6, and >10,000 nM, respectively). 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). In vivo, milnacipran (30 mg/kg) increases withdrawal threshold and latency in response to tactile and heat stimulation, respectively, in nerve-ligated mice. Formulations containing milnacipran have been used to treat fibromyalgia pain.Formal Name: (1R,2S)-rel-2-(aminomethyl)-N,N-diethyl-1-phenyl-cyclopropanecarboxamide, monohydrochloride. CAS Number: 101152-94-7. Synonyms: F 2207. Molecular Formula: C15H22N2O . HCl. Formula Weight: 282.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 33 mg/ml, Ethanol: 33 mg/ml, PBS (pH 7.2): 10 mg/ml. SMILES: NC[C@H]1C[C@]1(C(N(CC)CC)=O)C2=CC=CC=C2.Cl. InChi Code: InChI=1S/C15H22N2O.ClH/c1-3-17(4-2)14(18)15(10-13(15)11-16)12-8-6-5-7-9-12,/h5-9,13H,3-4,10-11,16H2,1-2H3,1H/t13-,15+,/m1./s1. InChi Key: XNCDYJFPRPDERF-PBCQUBLHSA-N.