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Local Anesthetic Agents lidocaine Powder,BP standard lidociane
Product Name: Lidocaine
Mol File: 137-58-6.mol
Lidocaine (Alphacaine)is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Histamine is responsible for many features of allergic reactions. Lidocaine (Alphacaine)is a second-generation antihistamine agent closely st
Antiarrhythmic Agents, Anesthetics
The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline.
Biological Activity Anasthetic and class Ib antiarrhythmic agent.? Blocks voltage-gated sodium channels in the inactivated state.
Local anesthetics Lidocaine is a local anesthetic, also known as Xylocaine, in recent years it has been replaced procaine, widely used in local infiltration anesthesia in cosmetic plastic surgery, it can block the nerve excitability and conduction by inhibiting the sodium channels of nerve cell membrane. The fat soluble and protein binding rate of lidocaine is higher than procaine, its cell penetrating ability is strong, fast onset, long duration of action, the interaction strength is 4 times of procaine.
Lidocaine is used in infiltration anesthesia, epidural anesthesia, topical anesthesia (including thoracoscopy or abdominal surgery for mucosal anesthesia) and nerve block. In order to extend the time of anesthesia, reduce the poisoning of lidocaine and other side effects, can be added in the anesthetic epinephrine.
Lidocaine can also be used for the treatment of ventricular premature beat after acute myocardial infarction, ventricular tachycardia, digitalis poisoning, cardiac surgery and cardiac catheterization-induced ventricular arrhythmias, including ventricular premature beats, ventricular tachycardia and ventricular fibrillation. Lidocaine is also used for duration status of epilepsy which other anti-seizure drugs are not effective, as well as local or spinal anesthesia. But it is usually ineffective for supraventricular arrhythmias.
Chemical property Lidocaine is white needle like crystals, and its melting point is 68-69℃; boiling point is 180-182℃ (0.53kPa), soluble in ethanol in 159-160℃ (0.267kPa), ether, benzene, chloroform and oil, do not dissolve in water. In common use radical hydrochloride, lidocaine hydrochloride (C14H22N2O • HCL, [73-78-9]) is a white crystalline powder. Melting point 127-129℃, and the monohydrate melting point is 77-78℃. Easily soluble in water, 0.5% aqueous solution pHO 4.0-5.5. Odorless, bitter taste.
Uses 1, This product is a local anesthetics of amide derivatives,and widely used in surface anesthesia, anesthesia, conduction anesthesia and epidural anesthesia. The LD50 of oral lidocaine hydrochloride to mice was 290 mg/kg.
2, Used as a local anesthetic.
Production method Lidocaine is derived from 2,6-dimethylaniline by acylation and amination. 1. Acylation:2,6-dimethylaniline dissolved in anhydrous benzene, cooled to 28℃ below, stirring and slowly dropping chloroacetyl chloride, controlling the temperature at 30℃ below. The reaction was then stirred for 1 h, and then heated to reflux 8h. Cooling, crystallizing, filtering and drying to obtain 2, 6-dimethyl chloroacetanilide, yield 75%. 2. Amination: added 2, 6-dimethyl chloroacetanilide to benzene, and then add diethylamine, stirring heated to reflux 7h. After recovery most of the benzene, cooling crystallization, filtration, washing crystallization with benzene. Combined with benzene liquid, extracted with 10% hydrochloric acid, added activated carbon decolorization in extract and filtered. Filtrate was adjusted to pH 10 with 10% sodium hydroxide solution, precipitation crystallization, rejection filter, washed to neutral, it was lidocaine. Recrystallization, salt with hydrochloric acid is the lidocaine hydrochloride. The yield of the amination reaction was 76%.
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