规格 | 价格 | 库存 | 数量 |
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50mg |
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100mg |
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Other Sizes |
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靶点 |
5-HT2B Receptor 11.2 nM (Ki) 5-HT2A Receptor 1516 nM (Ki) 5-HT2C Receptor 324 nM (Ki)
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体外研究 (In Vitro) |
在大鼠中,当暴露于 (+)-去甲芬氟拉明(1 nM 至 100 μM)时,阈值显着下降的动脉(肠系膜阻力动脉和主动脉)会收缩[1]。 (+)-去甲芬氟拉明(1 和 10 μM,3 分钟)可在正常血压和高血压大鼠的组织中诱导主动脉收缩[1]。当暴露于 (0–10 μM)-去甲芬氟拉明三分钟时,大鼠海马突触体以 Ca2+ 依赖性方式释放 5-HT [2]。
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体内研究 (In Vivo) |
在清醒的 SHAM 和 DOCA 盐大鼠中,(+)-去甲芬氟拉明(1-300 μg/kg,静脉注射)会产生升压反应[1]。 (+)-去甲芬氟拉明(2.5 和 5 mg/kg,腹腔注射)可降低大鼠端脑和脑干 5-HT 和 5-HIAA 水平[3]。
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动物实验 |
Animal/Disease Models: Conscious SHAM and DOCA-salt rats[1].
Doses: 1-300 μg/kg Route of Administration: intravenous (iv) injection (iv), given in a cumulative fashion at 6-min intervals. Experimental Results: Induced pressor response in conscious SHAM and DOCA-salt rats. (change in mean arterial blood pressure at 300 μg/kg, mm Hg, SHAM vehicle=36, SHAM ketanserin=7, DOCA=51, DOCA ketanserin=19). |
参考文献 |
[1]. Wei Ni, et al. The 5-hydroxytryptamine2A receptor is involved in (+)-norfenfluramine-induced arterial contraction and blood pressure increase in deoxycorticosterone acetate-salt hypertension. J Pharmacol Exp Ther. 2007 May;321(2):485-91.
[2]. M Gobbi, et al. In vitro studies on the mechanism by which (+)-norfenfluramine induces serotonin and dopamine release from the vesicular storage pool. Naunyn Schmiedebergs Arch Pharmacol. 1998 Sep;358(3):323-7. [3]. R Invernizzi, et al. Is receptor activation involved in the mechanism by which (+)-fenfluramine and (+)-norfenfluramine deplete 5-hydroxytryptamine in the rat brain? Br J Pharmacol. 1982 Mar;75(3):525-30. |
分子式 |
C10H12F3N
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分子量 |
203.20
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CAS号 |
19036-73-8
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相关CAS号 |
(+)-Norfenfluramine hydrochloride;37936-89-3;Norfenfluramine;1886-26-6
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SMILES |
FC(C1=CC=CC(=C1)C[C@H](C)N)(F)F
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溶解度 (体外) |
DMSO: 100 mg/mL (492.13 mM)
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (12.30 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 4.9213 mL | 24.6063 mL | 49.2126 mL | |
5 mM | 0.9843 mL | 4.9213 mL | 9.8425 mL | |
10 mM | 0.4921 mL | 2.4606 mL | 4.9213 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。