利多卡因（10 nM；48 小时）会显着降低细胞生长[2]。利多卡因（1-10 nM；24-72 小时）抑制细胞活力；在剂量为 10 nM 且治疗持续时间为 48 小时时获得最大抑制效果 [2]。利多卡因（10 nM；48 小时）可显着增加细胞凋亡率 [2]。利多卡因（10 nM；48 小时）可显着增加 p21 的表达并下调 Cyclin D1 [2]。

在大鼠中，利多卡因（lidocaine）产生完全可逆的尾部神经阻滞。与热伤害性阻断相比，由利多卡因产生的机械性伤害性阻断起效较慢且恢复较快[3]。

细胞增殖实验 [2]
细胞类型：人胃癌细胞系 MKN45
测试浓度： 10 nM
孵育时间：48小时
实验结果：细胞增殖急剧减弱。

---

细胞活力测定 [2]
细胞类型： 人胃癌细胞系 MKN45
测试浓度： 1、5 和 10 nM
孵育持续时间：24、48、72小时
实验结果：抑制MKN45细胞活力。

---

细胞凋亡分析 [2]
细胞类型： 人胃癌细胞系 MKN45
测试浓度： 10 nM
孵育时间：48小时
实验结果：细胞凋亡率急剧增加。

---

蛋白质印迹分析 [2]
细胞类型： 人胃癌细胞系 MKN45
测试浓度： 10 nM
孵育时间：48小时
实验结果：Cyclin D1表达显着下调，p21表达显着上调。

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Lidocaine concentrations in milk during continuous IV infusion, epidural administration and in high doses as a local anesthetic are low and the lidocaine is poorly absorbed by the infant. Lidocaine is not expected to cause any adverse effects in breastfed infants. No special precautions are required.
Lidocaine during labor and delivery with other anesthetics and analgesics has been reported by some to interfere with breastfeeding. However, this assessment is controversial and complex because of the many different combinations of drugs, dosages and patient populations studied as well as the variety of techniques used and deficient design of many of the studies. Overall it appears that with good breastfeeding support epidural lidocaine with or without fentanyl or one of its derivatives has little or no adverse effect on breastfeeding success. Labor pain medication may delay the onset of lactation.
◉ Effects in Breastfed Infants
Lidocaine in doses ranging from 60 to 500 mg administered to the mother by intrapleural or epidural routes during delivery had no effect on their 14 infants who were either breastfed or received their mother's breastmilk by bottle.
A neurology group reported using 1% lidocaine for peripheral nerve blocks in 14 nursing mothers with migraine. They reported no infant side effects and considered the procedure safe during breastfeeding.
◉ Effects on Lactation and Breastmilk
A randomized study compared three groups of women undergoing elective cesarean section who received subcutaneous infusion of 20 mL of lidocaine 1% plus epinephrine 1:100:000 at the incision site. One group received the lidocaine before incision, one group received the lidocaine after the incision, and the third received 10 mL before the incision and 10 mL after. Women in the pre-and post-incision administration group initiated breastfeeding earlier than those in the pre-incision administration (3.4 vs 4.1 hours). There was no difference between the post-incision administration group and the other groups in time to breastfeeding initiation.
A national survey of women and their infants from late pregnancy through 12 months postpartum compared the time of lactogenesis II in mothers who did and did not receive pain medication during labor. Categories of medication were spinal or epidural only, spinal or epidural plus another medication, and other pain medication only. Women who received medications from any of the categories had about twice the risk of having delayed lactogenesis II (>72 hours) compared to women who received no labor pain medication.
An Egyptian study compared lidocaine 2% (n = 75) to lidocaine 2% plus epinephrine 1:200,000 (n = 70) as a wound infiltration following cesarean section. Patients who received epinephrine in combination with lidocaine began breastfeeding at 89 minutes following surgery compared to 132 minutes for those receiving lidocaine alone. The difference was statistically significant.

[1]. Setting up for the block: the mechanism underlying lidocaine's use-dependent inhibition of sodium channels. J Physiol. 2007 Jul 1;582(Pt 1):11.

[2]. Lidocaine inhibits growth, migration and invasion of gastric carcinoma cells by up-regulation of miR-145. BMC Cancer. 2019 Mar 15;19(1):233.

[3]. Evaluation of the antinociceptive effects of lidocaine and bupivacaine on the tail nerves of healthy rats. Basic Clin Pharmacol Toxicol. 2013 Jul;113(1):31-6.

Lidocaine Hydrochloride is the hydrochloride salt form of lidocaine, an aminoethylamide and a prototypical member of the amide class anesthetics. Lidocaine interacts with voltage-gated Na+ channels in the nerve cell membrane and blocks the transient increase in permeability of excitable membranes to Na+. This prevents the generation and conduction of nerve impulses and produces a reversible loss of sensation. Lidocaine hydrochloride also exhibits class IB antiarrhythmic effects. The agent decreases the flow of sodium ions into myocardial tissue, especially on the Purkinje network, during phase 0 of the action potential, thereby decreasing depolarization, automaticity and excitability.
A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.
See also: Lidocaine Hydrochloride (annotation moved to).

C14H25CLN2O2

288.816

288.16

6108-05-0

Lidocaine;137-58-6

16219577

Typically exists as solid at room temperature

350.8ºC at 760 mmHg

68.5ºC

166ºC

3.394

41.57

3

3

5

19

228

0

O=C(C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])N([H])C1C(C([H])([H])[H])=C([H])C([H])=C([H])C=1C([H])([H])[H]

YECIFGHRMFEPJK-UHFFFAOYSA-N

InChI=1S/C14H22N2O.ClH/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4;/h7-9H, 5-6,10H2,1-4H3,(H,15,17);1H;

2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide;hydrate;hydrochloride;

Lidocaine Hydrochloride; LIDOCAINE HCL; Lidothesin; Lignocaine hydrochloride; Xyloneural; Xylocitin;

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。

---

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。

View More

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)

---

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。

View More

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

---

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。

---

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。