norepinephrine reuptake ( Ki = 8.2 nM )

体外活性：瑞波西汀（也称为 PNU 155950E；商品名：Edronax）是一种去甲肾上腺素再摄取抑制剂，Ki 为 8.2 nM，具有抗抑郁活性。瑞波西汀剂量依赖性且完全抑制人去甲肾上腺素转运蛋白的 [3H]-多巴胺摄取（ hNET），在 Madin–Darby 犬肾 (MDCK) 细胞中 Ki 值为 11 nM。瑞波西汀剂量依赖性地有效抑制大鼠蓝斑神经元放电，ED50 为 191 μg/kg。瑞波西汀对蓝斑神经元的抑制作用可被 α2 拮抗剂哌罗生（1.5 mg/kg，IV）逆转。瑞波西汀剂量依赖性地完全抑制人去甲肾上腺素转运蛋白 (hNET) 对 [3H]-多巴胺的摄取，在 Madin–Darby 犬肾 (MDCK) 细胞中 Ki 值为 11 nM。 激酶测定：瑞波西汀（也称为 PNU 155950E；贸易）名称：Edronax）是一种去甲肾上腺素再摄取抑制剂，Ki 为 8.2 nM，具有抗抑郁活性。细胞测定：瑞波西汀剂量依赖性且完全抑制人去甲肾上腺素转运蛋白 (hNET) 的 [3H]-多巴胺摄取，Madin 中的 Ki 值为 11 nM –达比犬肾 (MDCK) 细胞。瑞波西汀剂量依赖性地有效抑制大鼠蓝斑神经元放电，ED50 为 191 μg/kg。瑞波西汀对蓝斑神经元的抑制作用可被 α2 拮抗剂哌罗生（1.5 mg/kg，IV）逆转。瑞波西汀剂量依赖性地完全抑制人去甲肾上腺素转运蛋白 (hNET) 对 [3H]-多巴胺的摄取，在 Madin–Darby 犬肾 (MDCK) 细胞中 Ki 值为 11 nM。

瑞波西汀剂量依赖性地有效抑制大鼠蓝斑神经元放电，ED50 为 191 μg/kg。瑞波西汀对蓝斑神经元的抑制作用可被 α2 拮抗剂哌罗生（1.5 mg/kg，IV）逆转。瑞波西汀剂量依赖性地逆转利血平诱导的小鼠眼睑痉挛和体温过低。瑞波西汀还被发现可以剂量依赖性地拮抗可乐定引起的小鼠体温过低。瑞波西汀可逆转利血平诱导的大鼠眼睑痉挛和体温过低，ED50 分别为 10 mg/kg 和 3 mg/kg (po)。瑞波西汀可显着减少 DSM-III-R 惊恐障碍患者惊恐发作和恐惧症状的平均次数。瑞波西汀还可以改善汉密尔顿抑郁量表、霍普金斯症状检查表 90 和希恩残疾量表的分数。与安慰剂相比，瑞波西汀的复发率显着降低（22% vs. 56%），并且在复发性 DSM-III-R 重度抑郁症患者的长期治疗过程中维持缓解的累积概率更大。瑞波西汀可有效预防发作缓解后抑郁症状的复发。瑞波西汀（0.3 mg/kg-20 mg/kg）的急性全身给药剂量依赖性地增加大鼠额叶皮质中的细胞外去甲肾上腺素，同时对细胞外血清素没有影响。瑞波西汀 (20 mg/kg) 还会增加大鼠额叶皮层的细胞外多巴胺。长期服用瑞波西汀 14 天会导致大鼠额叶皮层细胞外去甲肾上腺素和多巴胺的基础浓度升高，细胞外去甲肾上腺素和多巴胺的净增加更大，但不会增加血清素。瑞波西汀剂量依赖性地减少尼古丁自我给药约 60%。瑞波西汀 (5.6 mg/kg) 的重复给药可降低 14 次疗程中的尼古丁自我给药和蔗糖维持反应。

细胞系：SH-SY5Y细胞
浓度：0.1 μM、1 μM、5 μM
孵育时间：24小时
结果：防止地塞米松引起的细胞活力和增殖率下降。

Harlan-bred, male CF-1 mice (18-20 g), depression models
3 mg/kg, 30 mg/kg
Intraperitoneal injection

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Reboxetine is not approved for marketing in the United States by the U.S. Food and Drug Administration, but is available in other countries. Limited information indicates that maternal doses of up to 10 mg daily produce low levels in milk and appear to not result in any adverse effects in breastfed infants. Until more data are available, reboxetine should be used with careful monitoring during breastfeeding.
◉ Effects in Breastfed Infants
Four infants whose mothers had postpartum depression had been breastfed (extent not stated) for 1.3 to 2.1 months during maternal reboxetine therapy at an average dose of 6.5 mg (79 mcg/kg) daily. One of the mothers was also taking escitalopram 20 mg daily and another was taking sertraline 300 mg daily. None of the infants exhibited any adverse reactions. Three of the infants had normal Denver developmental scores; the fourth whose mother was taking reboxetine had a developmental age of only 71% of normal, but the problem predated maternal reboxetine therapy.
Five women used reboxetine during pregnancy and lactation (extent not stated) in unspecified doses. No adverse effects were noted in their infants and normal developmental milestones were reported.
◉ Effects on Lactation and Breastmilk
Reboxetine increased serum prolactin in male subjects. The relevance of this finding to nursing mothers is not clear. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.
An observational study looked at outcomes of 2859 women who took an antidepressant during the 2 years prior to pregnancy. Compared to women who did not take an antidepressant during pregnancy, mothers who took an antidepressant during all 3 trimesters of pregnancy were 37% less likely to be breastfeeding upon hospital discharge. Mothers who took an antidepressant only during the third trimester were 75% less likely to be breastfeeding at discharge. Those who took an antidepressant only during the first and second trimesters did not have a reduced likelihood of breastfeeding at discharge. The antidepressants used by the mothers were not specified.
A retrospective cohort study of hospital electronic medical records from 2001 to 2008 compared women who had been dispensed an antidepressant during late gestation (n = 575) to those who had a psychiatric illness but did not receive an antidepressant (n = 1552) and mothers who did not have a psychiatric diagnosis (n = 30,535). Women who received an antidepressant were 37% less likely to be breastfeeding at discharge than women without a psychiatric diagnosis, but no less likely to be breastfeeding than untreated mothers with a psychiatric diagnosis. None of the mothers were taking reboxetine.
In a study of 80,882 Norwegian mother-infant pairs from 1999 to 2008, new postpartum antidepressant use was reported by 392 women and 201 reported that they continued antidepressants from pregnancy. Compared with the unexposed comparison group, late pregnancy antidepressant use was associated with a 7% reduced likelihood of breastfeeding initiation, but with no effect on breastfeeding duration or exclusivity. Compared with the unexposed comparison group, new or restarted antidepressant use was associated with a 63% reduced likelihood of predominant, and a 51% reduced likelihood of any breastfeeding at 6 months, as well as a 2.6-fold increased risk of abrupt breastfeeding discontinuation. Specific antidepressants were not mentioned.

[1]. Biol Psychiatry . 2000 May 1;47(9):818-29.

[2]. J Clin Psychiatry . 2002 Jan;63(1):31-7.

[3]. J Clin Psychiatry . 1999 Jun;60(6):400-6.

[4]. Neuropsychopharmacology . 2002 Aug;27(2):237-47.

[5]. J Pharmacol Exp Ther . 2002 Nov;303(2):664-72.

A morpholine derivative that is a selective and potent noradrenaline reuptake inhibitor; it is used in the treatment of DEPRESSIVE DISORDER.

C20H27NO6S

409.5

409.155

C, 58.66; H, 6.65; N, 3.42; O, 23.44; S, 7.83

98769-84-7

Reboxetine; 71620-89-8; (R,R)-Reboxetine mesylate; 105017-39-8

127150

White to off-white solid powder

443.7ºC at 760 mmHg

170-171ºC

188.2ºC

4.107

102.47

2

7

6

28

425

2

S(C([H])([H])[H])(=O)(=O)O[H].O1C([H])([H])C([H])([H])N([H])C([H])([H])[C@]1([H])[C@@]([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])OC1=C([H])C([H])=C([H])C([H])=C1OC([H])([H])C([H])([H])[H]

CGTZMJIMMUNLQD-STYNFMPRSA-N

InChI=1S/C19H23NO3.CH4O3S/c1-2-21-16-10-6-7-11-17(16)23-19(15-8-4-3-5-9-15)18-14-20-12-13-22-18;1-5(2,3)4/h3-11,18-20H,2,12-14H2,1H3;1H3,(H,2,3,4)/t18-,19-;/m1./s1

(2R)-2-[(R)-(2-ethoxyphenoxy)-phenylmethyl]morpholine;methanesulfonic acid

PNU 155950E; PNU155950E; PNU-155950E; FCE-20124 mesylate; PNU-155950E mesylate; FCE 20124 mesylate; PNU 155950E mesylate; FCE20124 mesylate; PNU155950E mesylate; Reboxetine mesilate; Reboxetine; Edronax; Reboxetine mesylate; Vestra (TN); AC1L2RIX; AC1Q6WCV; DSSTox_CID_25690; DSSTox_RID_81062; DSSTox_GSID_45690.

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: 82~125 mg/mL (200.2~305.3 mM)
Water: < 1 mg/mL
Ethanol: ~82 mg/mL (~200.2 mM)

配方 1 中的溶解度: ≥ 2.08 mg/mL (5.08 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.08 mg/mL (5.08 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.08 mg/mL (5.08 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 110 mg/mL (268.62 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
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。