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Levobupivacaine HCl(S-Bupivacaine)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Levobupivacaine HCl(S-Bupivacaine)图片
CAS NO:27262-48-2
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)324.89
FormulaC18H28N2O.HCl
CAS No.27262-48-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 64 mg/mL (197 mM)
Water: 64 mg/mL (197 mM)
Ethanol: 57 mg/mL (175.4 mM)
Other info

Chemical Name: (2S)-1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride

InChi Key: SIEYLFHKZGLBNX-NTISSMGPSA-N

InChi Code: InChI=1S/C18H28N2O.ClH/c1-4-5-12-20-13-7-6-11-16(20)18(21)19-17-14(2)9-8-10-15(17)3;/h8-10,16H,4-7,11-13H2,1-3H3,(H,19,21);1H/t16-;/m0./s1

SMILES Code: O=C([C@H]1N(CCCC)CCCC1)NC2=C(C)C=CC=C2C.[H]Cl

Synonyms(S)-(-)-Bupivacaine HCl; Levobupivacaine, Levobupivacaine HCl; Levobupivacaine hydrochloride; Chirocaine, Novabupi
实验参考方法
In Vitro

In vitro activity: Levobupivacaine is an amide-type local anaesthetic. Levobupivacaine acts via blockade of voltage-sensitive ion channels in neuronal membranes, preventing transmission of nerve impulses. Localised and reversible anaesthesia is produced by interference with the opening of the sodium channel, which inhibits conduction of the action potential in nerves involved in sensory and motor activity and sympathetic activity. Levobupivacaine displaces 3H-BTX from sodium channels of rat brain synaptosomes with IC50 of 2.9 μM and Hill coefficients of 1.2. When cell membrane is held at -80 mV, -70 mV, -60 mV or -100 mV, Levobupivacaine shows tonic inhibition of sodium channel in GH3 cells with IC50s of 132.1, 37.6, 21.6 and 264 μM, respectively. Levobupivacaine depresses action potential of isolated axon in vitro. Levobupivacaine (1mM) depresses action potential amplitude and maximal rate of rise of action potential (dV/dtmax) in the crayfish giant axons with value of 88 and 81 respectively, after perfusion for 15 min. Levobupivacaine also displays activity on cardiac ion channels. In isolated ventricular myocytes, the apparent affinity for inactivated state of the sodium channel is 4.8 μM for Levobupivacaine, with a calculated KD of 39μM. On inhibition of cardiac delayed rectifier potassium channels (hKv1.5), the steady-state block for Levobupivacaine (20 μM) is 31%, with a calculated KD of 27.3 μM. Levobupivacaine may also inhibit cardiac calcium channels. 10 μM Levobupivacaine produces a 50% decrease in contractile force of guinea-pig papillary muscles.

In VivoLevobupivacaine has similar nerve blocking potency with bupivacaine. Levobupivacaine at a dose of 0.125%, inhibits motor and nocifensive pinch responses with maximum %MPE of 99 and 68 respectively, and inhibits the duration of deficits of motor and nocifensive pinch responses (60 and 30 , respectively) after sciatic nerve block.
Animal model
Formulation & Dosage
References

Drugs. 2000 Mar;59(3):551-79; Anesthesiology. 2000 Sep;93(3):744-55; Expert Opin Investig Drugs. 1999 Jun;8(6):861-76.