盐酸丙咪嗪作用机制 - Medchemexpress - MCE中国

1、Product Data SheetImipramine hydrochlorideCat. No.: HY-B1490CAS No.: 113-52-0分式: CHClN分量: 316.87作靶点: Serotonin Transporter作通路: Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (315.59 mM)H2O : 62.5 mg/mL (197.24 mM; Need ultrasonic)*

2、means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 3.1559 mL 15.7793 mL 31.5587 mL5 mM 0.6312 mL 3.1559 mL 6.3117 mL10 mM 0.3156 mL 1.5779 mL 3.1559 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，

3、-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.89 mM); Clear solution此案可

4、获得 2.5 mg/mL (7.89 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.89 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (7.89 mM，饱和度未知)

5、的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.89 mM); Clear solution此案可获得 2.5 mg/mL (7.89 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活

6、性 Imipramine hydrochloride抑制素转运蛋(serotonin)，体内试验的IC50值为32 nM。IC & Target IC50: 32 nM (serotonin)1体外研究 Depression-like behavior is often complicated by chronic pain. Antidepressants including imipramine are widely usedto treat chronic pain, but the mechanisms are not fully understood2. Imipramine (IC

7、50=32 nM) and desipramine (IC50=160 nM) are found to be potent inhibitors of the human placental serotonin transporter1.体内研究 Administration of imipramine reverses social avoidance behavior, significantly increasing the interaction time. 24 daysof imipramine treatment in RSD mice significantly decrea

8、ses stress-induced mRNA levels for IL-6 in brain microglia3. Chronic mild stress induces a long-term altered gene expression profile in the prefrontal cortex that is partiallyreverted by imipramine treatment (10mg/kg, i.p.)4. Chronic imipramine administration alteres the amino aciddynamics in the br

9、ain. In the striatum, the concentrations of asparagine, glutamine and methionine are significantlyincreased by chronic imipramine administration. In the thalamus and hypothalamus, chronic imipramineadministration significantly decreased the valine concentration5. Imipramine reduces pain-related nega

10、tive emotionwithout influencing pain and that this effect is diminished by denervation of 5-HT neurons and by anti-BDNFtreatment. Imipramine also normalizes derangement of ERK/CREB coupling, which leads to induction of BDNF. Thissuggests a possible interaction between 5-HT and BDNF2. Imipramine trea

11、tment counteracts the corticosteroneadministration-induced increase in the reactivity of rat CA3 hippocampal circuitry to the activation of the 5-HTreceptor6.PROTOCOLAnimal Rats: The Wistar (WIS) and Wistar Kyoto (WKY) rats are divided into four groups: (1) a control WIS rat group, (2) anAdministrat

12、ion 35 imipramine-treated WIS rat group, (3) a control WKY rat group and (4) an imipramine-treated WKY rat group.Distilled water (10 mL/kg) or imipramine solution (10 mg/10 mL/kg) is orally administered for 28 days except on theday of the open field test, when nothing is administered in order to avo

13、id the acute effect of single administration onthe open field test5.Mice: C57BL/6 mice subjected to repeated social defeat (RSD), home cage control (HCC) are randomLy selected intofour groups: RSD/imipramine, RSD/vehicle, HCC/imipramine, and HCC/vehicle. Mice in the RSD/imipramine receiveddaily intr

14、aperitoneal (i.p.) injections of imipramine (20 mg/kg) for 24 days after the 6 cycles of RSD. HCC/imipraminereceived daily i.p. imipramine at the same dose while RSD/vehicle and HCC/vehicle groups received i.p. injections ofvehicle (sodium chloride, 0.9%) for 24 days at the same time point3.MCE has

15、not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemEREFERENCES1. Balkovetz DF, et al. Evidence for an imipramine-sensitive serotonin transporter in human placental brush-border membranes. J Biol Chem. 1989 Feb5;264(4):2195-8.2. Yasuda S, et

16、al. Imipramine ameliorates pain-related negative emotion via induction of brain-derived neurotrophic factor. Cell Mol Neurobiol. 2014Nov;34(8):1199-208.3. Ramirez K, et al. Imipramine attenuates neuroinflammatory signaling and reverses stress-induced social avoidance. Brain Behav Immun. 2015May;46:2

17、12-20.4. Erburu M, et al. Chronic mild stress and imipramine treatment elicit opposite changes in behavior and in gene expression in the mouse prefrontal cortex.Pharmacol BiochemBehav. 2015 Aug;135:227-36.5. Nagasawa M, et al. Chronic imipramine treatment differentially alters the brain and plasma amino acid metabolism in Wistar and Wistar Kyoto rats. Eur JPharmacol. 2015 Sep 5;762:127-35.6. Tokarski K, et al. Imipramine counteracts corticosterone-induced alterations in the effects of the activation of 5-HT(7) receptors in rat hippoc