Benzocaine shares a common receptor with all othe rLAs in the voltage-gated Na channel, with an IC 50 of 0.8 mM tested with a potential of +30 mV.
性状
Solid
IC50 & Target[1][2]
IC50: 0.8 mM (Na channel).
体外研究(In Vitro)
Benzocaine blocks μ1 wild-type Na currents in a dose-dependent Manner. The Benzocaine concentration that inhibits 50% of Na currents (IC50) is estimated to be about 0.8 mM when a test potential of +30 mV is applied. The slope of the h∞ curve is also significantly reduced by benzocaine (from 6.6 to 9.9 mV). Mutation of μ1-N1584A also significantly increases the potency of Benzocaine. At 1 mM, Benzocaine blocks about 55% of wild-type Na current but about 95% of μ1-N1584A mutant current. Benzocaine also appears to bind more strongly to its LA receptor in the N1584A mutant than in the wild type. The inhibition of Ca uptake occurres at lower Benzocaine concentration (IC50=40.3±1.2mM) than that affecting the enzymatic activity. has not independently confirmed the accuracy of these methods. They are for r
体内研究(In Vivo)
Benzocaine is topically applied to the following species: dogs, domestic shorthair cats, Long-Evans rats, Sprague-Dawley rats, ferrets, rhesus monkeys, cynomolgus monkeys, owl monkeys, New Zealand White rabbits, miniature pigs, ICR mice, C3H mice, and C57BL/10SnJ mice. All animals, except mice and rats, receive a 2-second spray to the mucous membranes of the nasopharynx for an estimated dose of 56 mg. A 2-second spray to rodents oral mucous membranes delivers too great a volume of fluid for these animals. The study is repeated in dogs several months later to confirm low response. Response to Benzocaine spray is observed in most animals tested, with response peaking between 15 and 30 minutes after dosing. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
ClinicalTrial
参考文献
[1]. Wang GK et al. A common local anesthetic receptor for benzocaine and etidocaine in voltage-gated mu1 Na+ channels. Pflugers Arch. 1998 Jan;435(2):293-302.[2]. Davis JA, et al. Benzocaine-induced methemoglobinemia attributed to topical application of the anesthetic in several laboratory animal species. Am J Vet Res. 1993 Aug;54(8):1322-6.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (605.36 mM)H2O : 2 mg/mL (12.11 mM; ultrasonic and warming and heat to 60°C)