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KI0795Lidocaine50 mg$154

Chemical Characteristic

Product NameLidocaine
SynonymsXylocaine, lignocaine
CAS No.137-58-6
Molecular Weight 234.34
FormulaC14H22N2O
Chemical Structure

Biological activities

Lidocaine is a local anesthetic and antiarrhythmic agent. Lidocaine prevents equilibrium [3H]BTXB binding to sodium channels present on freshly isolated rat cardiac myocytes with an IC50 of 61 µM.[1]Lidocaine increases the decay of whole-cell FQ currents in Xenopus oocytes, reestablishing the wild-type phenotype. Lidocaine blocks peak inward current at -20 mV with an IC50 of 513 µM. Lidocaine prevents plateau current with an IC50 of only 74 µM.[2] Lidocaine reverses histamine, acetylcholine, and depolarizing hypertonic potassium contractures with the median effective doses of 2.8, 6.0, and 3.2 mg.[3] Lidocaine blocks granulocyte adherence and inhibits granulocyte delivery to inflammatory sites.[4] Rats injected with 7.5% lidocaine develop degenerative lesions limited to the posterior roots.[5]

Protocols

In vivo: Lidocaine is dissolved in distilled water.[5]

References

[1] Hill RJ, et al. Class I antiarrhythmic drug receptor: biochemical evidence for state-dependent interaction with quinidine and lidocaine. Mol Pharmacol. 1989, 36(1): 150-159. 閵嗏偓閵嗏偓
[2] Balser JR, et al. Local anesthetics as effectors of allosteric gating. Lidocaine effects on inactivation-deficient rat skeletal muscle Na channels. J Clin Invest. 1996, 98(12): 2874-2886. 閵嗏偓閵嗏偓
[3] Weiss EB, et al. The effect of local anesthetic, lidocaine, on guinea pig trachealis muscle in vitro. Am Rev Respir Dis. 1975, 112(3): 393-400. 閵嗏偓閵嗏偓
[4] MacGregor RR, et al. Lidocaine inhibits granulocyte adherence and prevents granulocyte delivery to inflammatory sites. Blood. 1980, 56(2): 203- 209. 閵嗏偓閵嗏偓
[5] Takenami T, et al. Intrathecal lidocaine causes posterior root axonal degeneration near entry into the spinal cord in rats. Reg Anesth Pain Med. 2002, 27(1): 58-67. 閵嗏偓閵嗏偓

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