Mepivacaine Hydrochloride

别名: 盐酸卡波卡因;N-(2,6-二甲基苯基)-1-甲基-2-哌啶甲酰胺盐酸盐;盐酸甲哌卡因; 甲哌卡因盐酸盐; Mepivacaine HCL 盐酸甲哌卡因;Mepivacaine Hydrochloride 甲哌卡因盐酸盐;盐酸甲哌卡因 USP标准品;盐酸甲哌卡因 标准品;盐酸甲哌卡因中间体
目录号: V10571 纯度: ≥98%
Mepivacaine HCl 与神经元细胞膜上特定的电压门控钠通道结合,抑制钠内流和膜去极化。
Mepivacaine Hydrochloride CAS号: 1722-62-9
产品类别: New1
产品仅用于科学研究,不针对患者销售
规格 价格 库存 数量
500mg
1g
5g
Other Sizes

Other Forms of Mepivacaine Hydrochloride:

  • 地昔卡因
  • Mepivacaine
  • 4-Hydroxy Mepivacaine-d3
  • 3-Hydroxy Mepivacaine-d3
  • Mepivacaine-d3
  • N-Methyl mepivacaine-d6 iodide
点击了解更多
InvivoChem产品被CNS等顶刊论文引用
产品描述
Mepivacaine HCl 与神经元细胞膜上特定的电压门控钠通道结合,抑制钠内流和膜去极化。
生物活性&实验参考方法
体外研究 (In Vitro)
盐酸甲哌卡因通过与神经元细胞膜中特定的电压门控钠通道结合来抑制钠内流和膜去极化。这会导致可逆的感觉丧失以及神经冲动的开始和传导受阻。与其他局部麻醉剂相比,这种药物起效更快,持续时间也较短[2]。与普鲁卡因相比,盐酸甲哌卡因起效更快,中间作用时间更长[3]。盐酸甲哌卡因可优先阻断 Na(v)1.8,且依赖于使用,而 S(-)-布比卡因则优先阻断 TTX Na(+) 通道 [4]。
毒性/毒理 (Toxicokinetics/TK)
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation
There is currently no information regarding the use of mepivacaine during lactation. Given the low levels of other local anesthetics in breast milk, a single dose of mepivacaine during lactation is unlikely to have adverse effects on breastfed infants. However, other medications may be preferred, especially when breastfeeding newborns or preterm infants.
Mepivacaine administered to mothers as a local anesthetic during labor has been reported to affect initial breastfeeding behavior in some infants, but not weight gain in the first 5 days postpartum. Although research on mepivacaine is limited, it appears that with good breastfeeding support, epidural local anesthetics, whether or not combined with fentanyl or its derivatives, have little or no adverse effects on breastfeeding success. Labor analgesia may delay the onset of lactation. More research is needed to clarify the impact of mepivacaine use during labor on breastfeeding outcomes.
◉ Effects on Breastfed Infants
As of the revision date, no relevant published information was found.
◉ Effects on Lactation and Breast Milk
A study compared the effects of epidural analgesia using mepivacaine, bupivacaine, and lidocaine during normal labor. The results showed no difference in weight change among the three groups of breastfed infants in the first five days postpartum. Overall weight gain was within the normal range in all groups.
Of the six infants who received mepivacaine pudendal nerve block within one hour before delivery, four started breastfeeding later and had fewer initial milk volumes than 10 infants who did not receive anesthesia during delivery. The long-term consequences of these differences have not been reported.
A national survey of women and their infants from late pregnancy to 12 months postpartum compared the time to lactroogenesis II in mothers who received and did not receive analgesia during labor. Drug categories included: spinal or epidural anesthesia alone, spinal or epidural anesthesia combined with other drugs, and other analgesics alone. Women who received any type of labor analgesia were approximately twice as likely to experience a delay in the second stage of lactation (>72 hours) compared to women who did not receive labor analgesia.
参考文献

[1]. ECMO for Cardiac Rescue after Accidental Intravenous Mepivacaine Application. Case Rep Pediatr. 2012;2012:491692.

[2]. mepivacaine hydrochloride.

[3]. Pharmacokinetics of the enantiomers of mepivacaine after intravenous administration of the racemate in volunteers. Anesth Analg, 1997. 84(1): p. 85-9.

[4]. Leffler, A., J. Reckzeh, and C. Nau, Block of sensory neuronal Na+ channels by the secreolytic ambroxol is associated with an interaction with local anesthetic binding sites. Eur J Pharmacol, 2010. 630(1-3): p. 19-28.

其他信息
Mepivacaine hydrochloride is the hydrochloride salt of mepivacaine and is used as a local anesthetic. It is a piperidine carboxamide compound with local anesthetic effects. Its function is related to that of mepivacaine. Mepivacaine hydrochloride is the hydrochloride form of mepivacaine, an amide derivative with local anesthetic properties. At the injection site, mepivacaine hydrochloride acts by binding to specific sodium ion channels on the neuronal cell membrane, thereby inhibiting sodium ion influx. This leads to nerve impulse conduction blockade, ultimately resulting in loss of sensation. Mepivacaine is a local anesthetic with a chemical structure related to bupivacaine but pharmacologically related to lidocaine. It is suitable for infiltration anesthesia, nerve blocks, and epidural anesthesia. Mepivacaine is only effective when used locally in large doses and therefore should not be used via this route. (Excerpt from AMA Drug Evaluation, 1994, p. 168) See also: mepivacaine (with active fraction); levonorepinephrine; mepivacaine hydrochloride (component).
*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性
化学信息 & 存储运输条件
分子式
C15H23CLN2O
分子量
282.8089
精确质量
282.149
CAS号
1722-62-9
相关CAS号
(+)-Mepivacaine;24358-84-7;Mepivacaine;96-88-8
PubChem CID
66070
外观&性状
White to off-white solid powder
沸点
383.1ºC at 760 mmHg
熔点
255-257ºC (dec.)
闪点
185.5ºC
蒸汽压
4.52E-06mmHg at 25°C
LogP
3.539
tPSA
32.34
氢键供体(HBD)数目
2
氢键受体(HBA)数目
2
可旋转键数目(RBC)
2
重原子数目
19
分子复杂度/Complexity
282
定义原子立体中心数目
0
InChi Key
RETIMRUQNCDCQB-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H22N2O.ClH/c1-11-7-6-8-12(2)14(11)16-15(18)13-9-4-5-10-17(13)3;/h6-8,13H,4-5,9-10H2,1-3H3,(H,16,18);1H
化学名
N-(2,6-dimethylphenyl)-1-methylpiperidine-2-carboxamide;hydrochloride
HS Tariff Code
2934.99.9001
存储方式

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(例如氮气保护),避免吸湿/受潮和光照。
运输条件
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
溶解度数据
溶解度 (体外实验)
H2O : ~100 mg/mL (~353.59 mM)
溶解度 (体内实验)
配方 1 中的溶解度: 100 mg/mL (353.59 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。

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。
制备储备液 1 mg 5 mg 10 mg
1 mM 3.5359 mL 17.6797 mL 35.3594 mL
5 mM 0.7072 mL 3.5359 mL 7.0719 mL
10 mM 0.3536 mL 1.7680 mL 3.5359 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。

计算器

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度,具体如下:

  • 计算制备已知体积和浓度的溶液所需的化合物的质量
  • 计算将已知质量的化合物溶解到所需浓度所需的溶液体积
  • 计算特定体积中已知质量的化合物产生的溶液的浓度
使用摩尔浓度计算器计算摩尔浓度的示例如下所示:
假如化合物的分子量为350.26 g/mol,在5mL DMSO中制备10mM储备液所需的化合物的质量是多少?
  • 在分子量(MW)框中输入350.26
  • 在“浓度”框中输入10,然后选择正确的单位(mM)
  • 在“体积”框中输入5,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案17.513 mg出现在“质量”框中。以类似的方式,您可以计算体积和浓度。

稀释计算器可计算如何稀释已知浓度的储备液。例如,可以输入C1、C2和V2来计算V1,具体如下:

制备25毫升25μM溶液需要多少体积的10 mM储备溶液?
使用方程式C1V1=C2V2,其中C1=10mM,C2=25μM,V2=25 ml,V1未知:
  • 在C1框中输入10,然后选择正确的单位(mM)
  • 在C2框中输入25,然后选择正确的单位(μM)
  • 在V2框中输入25,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案62.5μL(0.1 ml)出现在V1框中
g/mol

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成,具体如下:

注:化学分子式大小写敏感:C12H18N3O4  c12h18n3o4
计算化合物摩尔质量(分子量)的说明:
  • 要计算化合物的分子量 (摩尔质量),请输入化学/分子式,然后单击“计算”按钮。
分子质量、分子量、摩尔质量和摩尔量的定义:
  • 分子质量(或分子量)是一种物质的一个分子的质量,用统一的原子质量单位(u)表示。(1u等于碳-12中一个原子质量的1/12)
  • 摩尔质量(摩尔重量)是一摩尔物质的质量,以g/mol表示。
/

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

  • 输入试剂的质量、所需的配液浓度以及正确的单位
  • 单击“计算”按钮
  • 答案显示在体积框中
动物体内实验配方计算器(澄清溶液)
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶/难溶于水的化合物),不同的产品和批次配方组成不同,如对配方有疑问,可先联系我们提供正确的体内实验配方。此外,请注意这只是一个配方计算器,而不是特定产品的确切配方。
+
+
+

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) 。

临床试验信息
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04561921 Unknown status Drug: Magnesium sulfate
Drug: Mepivacaine-Levonordefrin Hydrochloride
Success of Inferior Alveolar Nerve Block Cairo University 2020-10-22 Not Applicable
NCT03725579 Unknown status Drug: mepivicane hydrochloride
Drug: articane hydrochloride
Symptomatic Irreversible Pulpitis Cairo University 2018-09-15 Phase 2
Phase 3
NCT04822415 Completed Drug: Mepivacaine
Drug: Articaine
Symptomatic Irreversible Pulpitis Cairo University 2014-12 Not Applicable
NCT04947267 Completed Drug: 3% Mepivacaine Hydrochloride
Drug: 2% Mepivacaine with 1:100,000 epinephrine
LOCAL ANESTHESIA Afshan Amjad Ali 2018-05-30 Phase 2
NCT05765682 Completed Other: Mepivacaine Spinal
Other: Bupivacaine Spinal
Total Knee Replacement Medical University of South Carolina 2023-03-13 Not Applicable
相关产品
联系我们