在 SK-N-SH 细胞中，nevopam（0.1-100 µM；15 分钟）以浓度依赖性方式抑制 22Na 吸收[1]。

Nefopam（0-10 mg/kg；静脉注射；单次）可保护小鼠免受电击引起的癫痫发作[1]。在长春新碱诱导的周围神经病变模型中，奈韦罗泮（10、30、60 mg/kg；腹腔注射；单次）表现出剂量依赖性的机械异常性疼痛减轻和神经激肽 -1 受体浓度下降[2]。

细胞活力测定[1]
细胞类型： SK-N-SH 细胞
测试浓度： 0.1 -100 µM
孵育时间： 15 分钟（预孵育）
实验结果： 抑制 22Na 的摄取，IC50 值为 27 µM。

Animal/Disease Models: Adult male NMRI mice (25-30 g; 6 to7weeks old; electroshock-induced seizures model)[1]
Doses: 0-10 mg /kg
Route of Administration: intravenous (iv) injection; single
Experimental Results: Produced dose-dependent protection against maximal electroshock seizures in mice with an ED50 of 3.8 (2.9-5.1) mg/kg.

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Animal/Disease Models: Adult male mice (10weeks old; 25- 30 g; vincristine-induced peripheral neuropathy model)[2].
Doses: 10, 30, 60 mg/kg
Route of Administration: intraperitoneal (ip) injection; single
Experimental Results: Dramatically diminished the percentage of NK1 receptors in the spinal cord at dosage of 60 mg/kg. demonstrated a sustained increase in paw withdrawal threshold against mechanical stimuli.

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Nefopam is not approved in the United States by the Food and Drug Administration. The amount of nefopam in breastmilk with usual maternal dosages is small. Nefopam does not appear to adversely affect the milk supply or the neurobehavioral scores of breastfed neonates. Breastfeeding is acceptable during maternal use of nefopam, although some recommend not using it after 48 hours postpartum.
◉ Effects in Breastfed Infants
Sixty-six women who had cesarean section deliveries were two groups postpartum: intravenous (IV) nefopam 20 mg every 6 hours or IV acetaminophen 1 gram every 6 hours as well as IV ketoprofen 50 mg every 6 hours in both groups Neonatal neurobehavioral scores were recorded at 12, 24, 48, and 72 hours post-caesarean by a pediatrician blinded to the group allocation. No difference was found between the groups in the behavioral scores.
◉ Effects on Lactation and Breastmilk
Sixty-six women who had cesarean section deliveries were two groups: IV nefopam 20 mg every 6 hours or IV acetaminophen 1 gram every 6 hours. All women received the same preoperative analgesia consisting of spinal bupivacaine, sufentanil, and morphine as well as intravenous ephedrine and phenylephrine to prevent hypotension. Postoperatively, all received IV oxytocin by infusion and IV ketoprofen 50 mg every 6 hours. Milk production was assessed by weighing the newborn before and after each breastfeed on days 2 and 3. No statistical differences were seen between the two groups in the weight difference before and after each feed, the newborn daily weight curve evolution, or the fall in weight between days 0 and 2. Mothers also rated their breast fullness to assess the onset of lactogenesis II; no difference was found between the two groups in the time to lactogenesis II. There was also no difference in serum prolactin between the groups.

[1]. Nefopam blocks voltage-sensitive sodium channels and modulates glutamatergic transmission in rodents. Brain Res. 2004 Jul 9;1013(2):249-55.

[2]. The Antiallodynic Effect of Nefopam on Vincristine-Induced Neuropathy in Mice. J Pain Res. 2020 Feb 7;13:323-329.

[3]. Rediscovery of nefopam for the treatment of neuropathic pain. Korean J Pain. 2014 Apr;27(2):103-11.

5-methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine is a member of the class of benzoxazocines that is 3,4,5,6-tetrahydro-1H-2,5-benzoxazocine substituted by phenyl and methyl groups at positions 1 and 5 respectively. It is a benzoxazocine and a tertiary amino compound.
Nefopam is under investigation for the prevention of Cholecystitis and Post Anaesthetic Shivering. Nefopam has been investigated for the prevention of Kidney Transplantation.
Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26)
See also: Nefopam Hydrochloride (annotation moved to).

C17H19NO

253.34

253.146

13669-70-0

Nefopam hydrochloride;23327-57-3

4450

Typically exists as solid at room temperature

1.1±0.1 g/cm3

369.5±37.0 °C at 760 mmHg

109.0±28.8 °C

0.0±0.8 mmHg at 25°C

1.564

3.44

12.47

0

2

1

19

274

0

CN1CCOC(C2=CC=CC=C2)C3=CC=CC=C3C1

RGPDEAGGEXEMMM-UHFFFAOYSA-N

InChI=1S/C17H19NO/c1-18-11-12-19-17(14-7-3-2-4-8-14)16-10-6-5-9-15(16)13-18/h2-10,17H,11-13H2,1H3

5-methyl-1-phenyl-1,3,4,6-tetrahydro-2,5-benzoxazocine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

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

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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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。