product name Levobupivacaine HCl
Description: Levobupivacaine HCl [also known as (S)-(-)-Bupivacaine HCl], the pure S(-)-enantiomer of bupivacaine, is a reversible neuronal sodium channel inhibitor, it is used as a long-acting local anesthetic. Levobupivacaine is an amide-type local anaesthetic that acts via blockade of voltage-sensitive ion channels in neuronal membranes, preventing transmission of nerve impulses.
References: Drugs. 2000;59(3):551-79; Anesthesiology. 2000;93(3):744-55; Expert Opin Investig Drugs. 1999;8(6):861-76.
324.89
Formula
C18H28N2O.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)
Solubility (In vivo)
Synonyms
(S)-(-)-Bupivacaine HCl
other peoduct :
| 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Levobupivacaine 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. |
