Local Anesthetic Drugs Levobupivacaine Hydrochloride / CAS 27262-48-2 Levobupivacaine HCl

Local Anesthetic Drugs Levobupivacaine Hydrochloride / CAS 27262-48-2 Levobupivacaine HCl

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Product NameLevobupivacaine Hydrochloride / Levobupivacaine HCL
SynonymsTIMTEC-BB SBB001337;(S)-(-)-BUPIVACAINE HCL;(S)-(-)-BUPIVACAINE HYDROCHLORIDE;(S)-(-)-1-N-BUTYL-2',6'-DIMETHYL-2-PIPERIDINCARBOXANILID HYDROCHLORIDECAS
CAS27262-48-2
Levobupivacaine HCL MFC18H29ClN2O
Levobupivacaine HCL MW324.89
Product CategoriesPharmaceutical Raw Materials;Active Pharmaceutical Ingredients
Levobupivacaine Hydrochloride MP254 °C (dec.)(lit.)
Levobupivacaine Hydrochloride AppearanceWhite powders
Chemical Propertieswhite crystalline powder
Applicationlevobupivacaine is amide local anesthetics
Min.Order1Kg Levobupivacaine HCL Available
PackingAluminum Foil Bag or Fiber Drum(1Kg, 25Kg)
Delivery MethodHKEMS, DHL, TNT, UPS, FEDEX, EMS etc. By air or by Sea.
Delivery Time5-14 Working Days, Tracking Number Available
Payment TermsT/T, MoneyGram, Western Union and Bitcoin
OriginHubei Province, China
Production CapacityLevobupivacaine HCL 500Kg/Month

Description:
Levobupivacaine (rINN) is a local anaesthetic drug belonging to the amino amide group. It is the S-enantiomer of bupivacaine.


The hydrochloride salt of levobupivacaine, an amide derivative with anesthetic property. Levobupivacaine reversibly binds voltage-gated sodium channels to modulate ionic flux and prevent the initiation and transmission of nerve impulses (stabilizing neuronal membrane), thereby resulting in analgesia and anesthesia. In comparison with racemic bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action.
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. [1] 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. [2] 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. [3] 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.


Levobupivacaine is a local anaesthetic drug belonging to the amino amide group. It is the S-enantiomer of bupivacaine,it is a reversible neuronal sodium channel inhibitor, used as a long-acting local anesthetic.
Levobupivacaine hydrochloride is commonly marketed by Abbott under the trade name Chirocaine.
Compared to bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action. It is approximately 13 percent less potent (by molarity) than racemic bupivacaine and has a longer motor block onset time.
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. [3] 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.
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.


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