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Crotamiton

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Chemical Structure| 483-63-6 同义名 : N-Ethyl-o-Crotonotoluidide
CAS号 : 483-63-6
货号 : A180524
分子式 : C13H17NO
纯度 : 95%
分子量 : 203.28
MDL号 : MFCD00026989
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 135 mg/mL(664.11 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 120 mg/mL(590.32 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Crotamiton is the only scabicide available today which displays not only antiprurtic but also marked antibacterial properties. It is especially indicated in the treatment of scabies in children as they are very prone to secondary bacterial infection following scratching[3]. Scabies is a relatively contagious infection caused by a tiny mite (Sarcoptes scabiei). Treatment with crotamiton 10% cream was effective in 46.8% of patients at the two-week follow-up, which increased to 62.5% at the four-week follow-up after this treatment was repeated[4]. Crotamiton strongly inhibited TRPV (vanilloid) 4 channels followed by large currents after crotamiton washout. In mice, crotamiton inhibited itch-related behaviors induced by a TRPV4-selective agonist (GSK1016790A)[5]. Topical application of 10% crotamiton moderately inhibited histamine-, serotonin-, and PAR-2 agonist-induced scratching behaviors. In addition, the antipruritic effects of crotamiton and corticosteroid appear to be, at least partly, associated with a TRPV1-independent pathway[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.92mL

0.98mL

0.49mL

24.60mL

4.92mL

2.46mL

49.19mL

9.84mL

4.92mL

参考文献

[1]Kittaka H, Yamanoi Y, Tominaga M. Transient receptor potential vanilloid 4 (TRPV4) channel as a target of crotamiton and its bimodal effects. Pflugers Arch. 2017 Jun 13.

[2]Izumoto S, Machida Y, et al. Chromatography of crotamiton and its application to the determination of active ingredients in ointments. J Pharm Biomed Anal. 1997 Jun;15(9-10):1457-66.

[3]Konstantinov D, Stanoeva L, Yawalkar SJ. Crotamiton cream and lotion in the treatment of infants and young children with scabies. J Int Med Res. 1979;7(5):443‐448

[4]Goldust M, Rezaee E, Raghifar R. Comparison of oral ivermectin versus crotamiton 10% cream in the treatment of scabies. Cutan Ocul Toxicol. 2014;33(4):333‐336

[5]Kittaka H, Yamanoi Y, Tominaga M. Transient receptor potential vanilloid 4 (TRPV4) channel as a target of crotamiton and its bimodal effects. Pflugers Arch. 2017;469(10):1313‐1323

[6]Sekine R, Satoh T, Takaoka A, Saeki K, Yokozeki H. Anti pruritic effects of topical crotamiton, capsaicin, and a corticosteroid on pruritogen-induced scratching behavior. Exp Dermatol. 2012;21(3):201‐204