S80886 |
Dasotraline hydrochloride (SEP-225289 hydrochloride) |
源葉(MedMol) | 99% |
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- 產(chǎn)品描述: Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
- 靶點(diǎn): IC50: 4 nM (dopamine), 6 nM (norepinephrine), 11 nM (serotonin);DopamineReceptor;5-HTReceptor;SerotoninTransporter;Norepinephrine
- 體內(nèi)研究:
Acute administration of dasotraline dose-dependently decreases the spontaneous firing rate of LC NE, VTA DA and DR 5-HT neurons through the activation of α2, D2 and 5-HT1A autoreceptors, respectively. Dasotraline predominantly inhibits the firing rate of LC NE neurons while producing only a partial decrease in VTA DA and DR 5-HT neuronal discharge. SEP-225289 is equipotent at inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a 50% recovery of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibition induced by microiontophoretic application of 5-HT and NE. Average dopamine and serotonin transporter occupancies increase with increasing doses of SEP-225289. Mean dopamine and serotonin transporter occupancies are 33%±11% and 2%±13%, respectively, for 8 mg; 44%±4% and 9%±10%, respectively, for 12 mg; and 49%±7% and 14%±15%, respectively, for 16 mg
- 參考文獻(xiàn):
1. Guiard BP, et al. Characterization of the electrophysiological properties of triple reuptake inhibitors on monoaminergic neurons. Int J Neuropsychopharmacol. 2011 Mar;14(2):211-23. 2. DeLorenzo C, et al. SEP-225289 serotonin and dopamine transporter occupancy: a PET study.
- 溶解性: Soluble in DMSO、H2O
- 保存條件: 2-8℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 3.043 ml 15.213 ml 30.427 ml 5 mM 0.609 ml 3.043 ml 6.085 ml 10 mM 0.304 ml 1.521 ml 3.043 ml 50 mM 0.061 ml 0.304 ml 0.609 ml
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)