Lidocaine-d10
(Synonyms: 利多卡因 d10) 目录号 : GC49525An internal standard for the quantification of lidocaine
Cas No.:851528-09-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Lidocaine-d10 is intended for use as an internal standard for the quantification of lidocaine by GC- or LC-MS. Lidocaine is an inhibitor of voltage-gated sodium channels (Navs) and a local anesthetic.1,2,3 It inhibits Nav1.2 (Ki = 11 µM), adult and neonatal Nav1.5 (IC50s = 380.1 and 360 µM, respectively), and Nav1.7 and Nav1.8 channels (IC50s = 450 and 104 µM, respectively) expressed in Xenopus oocytes. Topical administration of lidocaine (1-2%) reduces escape behavior in a rhesus monkey model of noxious electrical cutaneous pain.4 Formulations containing lidocaine have been used as local and regional anesthetics.
1.Ragsdale, D.S., McPhee, J.C., Scheuer, T., et al.Common molecular determinants of local anesthetic, antiarrhythmic, and anticonvulsant block of voltage-gated Na+ channelsProc. Natl. Acad. Sci. USA93(17)9270-9275(1996) 2.Fraser, S.P., Onkal, R., Theys, M., et al.Neonatal Nav1.5 channels: Pharmacological distinctiveness of a cancer-related voltage-gated sodium channel splice variantBr. J. Pharmacol.Online ahead of print(2021) 3.Chevrier, P., Vijayaragavan, K., and Chahine, M.Differential modulation of Nav1.7 and Nav1.8 peripheral nerve sodium channels by the local anesthetic lidocaineBr. J. Pharmacol.142(3)576-584(2004) 4.Lineberry, C.G., and Kulics, A.T.The effects of diazepam, morphine and lidocaine on nociception in rhesus monkeys: A signal detection analysisJ. Pharmacol. Exp. Ther.205(2)302-310(1978)
Cas No. | 851528-09-1 | SDF | Download SDF |
别名 | 利多卡因 d10 | ||
Canonical SMILES | [2H]C([2H])([2H])C([2H])([2H])N(C([2H])([2H])C([2H])([2H])[2H])CC(N(C1=C(C)C=CC=C1C)[H])=O | ||
分子式 | C14H12D10N2O | 分子量 | 244.4 |
溶解度 | DMSO: soluble | 储存条件 | -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 4.0917 mL | 20.4583 mL | 40.9165 mL |
5 mM | 0.8183 mL | 4.0917 mL | 8.1833 mL |
10 mM | 0.4092 mL | 2.0458 mL | 4.0917 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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HPLC-MS/MS measurement of lidocaine in rat skin and plasma. Application to study the release from medicated plaster
J Chromatogr B Analyt Technol Biomed Life Sci 2020 Feb 1;1138:121942.PMID:31918305DOI:10.1016/j.jchromb.2019.121942
A simple, sensitive HPLC-MS/MS method was developed and validated for the determination of lidocaine in skin and plasma of rats. The methods were established and validated assessing lower limit of quantitation (LLOQ), linearity, intra and inter-day precision and accuracy, selectivity, recovery and matrix effect. Chromatography was done on a Gemini column embedded with C18 stationary phase (50 mm × 2.0 mm, 5 µm particle size), using a gradient with mobile phases consisting of 0.1% HCOOH in bidistilled water and 0.1% HCOOH in acetonitrile. The mass spectrometer worked with electrospray ionization in positive ion mode and selected reaction monitoring, using target ions m/z 235.10 for lidocaine and m/z 245.10 for Lidocaine-d10, used as internal standard. RESULTS: The linearity of the method was in the ranges of lidocaine concentrations 10.0-200.0 ng/mL for skin homogenate (accuracy 94.1-105.5%; R2 ≥ 0.998) and 0.025-2 ng/mL for plasma (accuracy 96.2-104.8%; R2 ≥ 0.996). The intra- and inter-day precision and accuracy determined on three quality control samples (20, 75 and 170 ng/mL for skin and 0.075, 0.4 and 1.5 ng/mL for plasma) were ≤4.2% and 103.8-108.2% for skin and ≤12.4% and 95.5-101.4% for plasma. The LLOQ was 10 ng/mL in skin homogenate and 0.025 ng/mL in plasma. The applicability of the method was demonstrated by measuring lidocaine in skin and plasma after exposure to medicated patches containing 5% lidocaine.