| 包装: | 1mg |
| 规格: | 98% |
| 市场价: | 5111元 |
| 分子量: | 287.8 |
Background:
Milnacipran-d5is intended for use as an internal standard for the quantification of milnacipran by GC- or LC-MS. Milnacipran is an orally bioavailable serotonin and norepinephrine reuptake inhibitor (SNRI).1It 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 and norepinephrine uptake over dopamine uptake in rat cerebral cortical synaptosomes (IC50s = 28.0, 29.6, and >10,000 nM, respectively).2Milnacipran is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3Aas 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).2,3In vivo, milnacipran (30 mg/kg) increases withdrawal threshold and latency in response to tactile and heat stimulation, respectively, in nerve-ligated mice.4Formulations containing milnacipran have been used in the treatment of fibromyalgia pain.
1.Chen, C., Dyck, B., Fleck, B.A., et al.Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitorsBioorg. Med. Chem.18(4)1346-1349(2008) 2.Mochizuki, D., Tsujita, R., Yamada, S., et al.Neurochemical and behavioural characterization of milnacipran, a serotonin and noradrenaline reuptake inhibitor in ratsPsychopharmacology (Berl)162(3)323-332(2002) 3.Ueta, K., Suzuki, T., Uchida, I., et al.In vitro inhibition of recombinant ligand-gated ion channels by high concentrations of milnacipranPsychopharmacology (Berl)175(2)241-246(2004) 4.Suzuki, T., Ueta, K., Tamagaki, S., et al.Antiallodynic and antihyperalgesic effect of milnacipran in mice with spinal nerve ligationAnesth. Analg.106(4)1309-1315(2008)
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