|(E)-2-(3-(吡咯烷-1-基)-1-(对甲苯基)丙烷-1-烯-1-基)吡啶盐酸盐水合物|CsnPharm

CAS No.: 6138-79-0

Triprolidine HCl monohydrate/盐酸曲普利啶一水合物 Catalog No. CSN21872

Synonyms: Actidilat;Pro-Actidil;Pro-Entra

Triprolidine Hydrochloride is the first generation histamine H1 antagonist used in allergic rhinitis.

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生物活性

描述Triprolidine HCl is a hydrochloride resulting from the formal reaction of equimolar amounts of triprolidine and hydrogen chloride. Its monohydrate is used for the symptomatic relief of uticaria, rhinitis, and various pruritic skin disorders. It has a role as a H1-receptor antagonist. It contains a triprolidine(1+). The absolute oral bioavailability of triprolidine (1-mg/kg dose) in the dog was low (4%). A comparison of triprolidine pharmacokinetic parameters in dogs, rabbits, rats, and humans revealed considerable similarity in elimination characteristics in these species^[1]. of 0, 250, 1000, or 2000 ppm (as the free base) to groups of 60 Fischer 344 (F344) rats of each sex for up to 2 years to evaluate its potential carcinogenicity. Survival was significantly extended in triprolidine-treated males and females, particularly at the high dose. At the close of the study high-dose males and females had gained significantly less body weight than controls. Triprolidine was not carcinogenic in F344 rats^[2]. The permeation rate of triprolidine in the stripped skin was greatly larger than that in the whole skin. The permeability of triprolidine was markedly increased with stripping of the mouse skin to remove the stratum corneum that acts as a barrier of skin permeation^[3].
参考文献

[1] Findlay JW, Butz RF, Coker GG, DeAngelis RL, Welch RM. Triprolidine radioimmunoassay: disposition in animals and humans. J Pharm Sci. 1984 Oct;73(10):1339-44
[2] Greenman DL, Sheldon W, Schieferstein G, Allen R, Allaben WT. Triprolidine: 104-week feeding study in rats. Fundam Appl Toxicol. 1995 Sep;27(2):223-31
[3] Shin SC, Lee HJ. Enhanced transdermal delivery of triprolidine from the ethylene-vinyl acetate matrix. Eur J Pharm Biopharm. 2002 Nov;54(3):325-8

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0042 mL
- 15.0210 mL
- 30.0420 mL
- 5 mM
- 0.6008 mL
- 3.0042 mL
- 6.0084 mL
- 10 mM
- 0.3004 mL
- 1.5021 mL
- 3.0042 mL

技术信息

CAS号

6138-79-0

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H25ClN2O

运输

蓝冰

分子量

332.87

别名

Actidilat;Pro-Actidil;Pro-Entra;Venen;Entra;Actidilon;Triprolidine HCl;盐酸曲普利啶一水合物

溶解度

DMSO	320.0 mg/mL (961.3 mM)
Water	260.0 mg/mL (781.1 mM)

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Triprolidine HCl monohydrate/盐酸曲普利啶一水合物 Catalog No. CSN21872

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