A neuropeptide with diverse biological activities
货号:ajcx22956
CAS:N/A
分子式:C15H17D5N2O.HCl
分子量：287.8
溶解度:DMSO: Soluble,Methanol: Soluble
纯度：98%
存储：Store at -20°C
库存：现货

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-HT_3Aas 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 (K_is = >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)