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| | Milnacipran-d5 (hydrochloride) Basic information |
| | Milnacipran-d5 (hydrochloride) Chemical Properties |
| solubility | DMSO: Soluble Methanol: Soluble |
| | Milnacipran-d5 (hydrochloride) Usage And Synthesis |
| Description | 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).1 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).2 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).2,3 In vivo, milnacipran (30 mg/kg) increases withdrawal threshold and latency in response to tactile and heat stimulation, respectively, in nerve-ligated mice.4 Formulations containing milnacipran have been used in the treatment of fibromyalgia pain.WARNING This product is not for human or veterinary use. | | References | [1] CHEN CHEN . Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors[J]. Bioorganic & Medicinal Chemistry Letters, 2008, 18 4: Pages 1346-1349. DOI: 10.1016/j.bmcl.2008.01.011 [2] D. MOCHIZUKI. Neurochemical and behavioural characterization of milnacipran, a serotonin and noradrenaline reuptake inhibitor in rats[J]. Psychopharmacology, 2002, 162 1: 323-332. DOI: 10.1007/s00213-002-1111-5 [3] KAZUYOSHI UETA. In vitro inhibition of recombinant ligand-gated ion channels by high concentrations of milnacipran.[J]. Psychopharmacology, 2004, 175 2: 241-246. DOI: 10.1007/s00213-004-1808-8 [4] TAKAHIRO SUZUKI. Antiallodynic and antihyperalgesic effect of milnacipran in mice with spinal nerve ligation.[J]. Anesthesia and analgesia, 2008, 106 4: 1309-1315, table of contents. DOI: 10.1213/ane.0b013e318167889a |
| | Milnacipran-d5 (hydrochloride) Preparation Products And Raw materials |
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