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Quinine hydrochloride dihydrate

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Chemical Structure| 6119-47-7 同义名 : 奎宁单盐酸盐二水合物 ;Quinine HCl Dihydrate
CAS号 : 6119-47-7
货号 : A244479
分子式 : C20H29ClN2O4
纯度 : 98%
分子量 : 396.908
MDL号 : MFCD00151248
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(264.54 mM)，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: 20 mg/mL(50.39 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
靶点

  • Potassium Channel
描述 Quinine Hydrochloride Dihydrate is a natural white crystalline alkaloid having antipyretic (fever-reducing), antimalarial, analgesic (painkilling), anti-inflammatory properties and a bitter taste. In patients with cerebral malaria receiving the standard dose of 10 mg/kg every eight hours, plasma quinine concentrations consistently exceeded 10 mg/liter, reaching a peak 60 +/- 25 hours (mean +/- 1 S.D.) after treatment was begun and then declining[3]. All field isolates exhibited higher IC50 values of CQ (chloroquine diphosphate), quinine hydrochloride dihydrate and DHA (dihydro-artemisinin) compared to reference strains. The resistance index of field isolates with respect to 3D7 ranged between 260.55 and 403.78 to CQ, 39.83 and 46.42 to quinine, and 2.98 and 4.16 to DHA[4]. In a multilevel Poisson regression model adjusted for sex, age, ADL(activities of daily living), smoking status, drinking status, number of medications used, use of medication for hypertension and diabetes and flow rate of saliva, subjects with low sensitivity (>0·003% quinine hydrochloride dihydrate) to bitter taste had a significant 1·70 times higher prevalence ratio (95% confident interval 1·04-2·80) for underweight compared with those with high sensitivity (0·0001% quinine hydrochloride dihydrate) [5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01289561 Alcohol or Other Drugs Effects Phase 1 Completed - United States, Maryland ... 展开 >> Behavioral Pharmacology Research Unit Baltimore, Maryland, United States, 21224 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.60mL

2.52mL

1.26mL

25.19mL

5.04mL

2.52mL
参考文献

[1]Srinivas M, Hopperstad MG, et al. Quinine blocks specific gap junction channel subtypes. Proc Natl Acad Sci U S A. 2001 Sep 11;98(19):10942-7.

[2]Gantner F, Uhlig S, et al. Quinine inhibits release of tumor necrosis factor, apoptosis, necrosis and mortality in a murine model of septic liver failure. Eur J Pharmacol. 1995 Dec 27;294(1):353-5.

[3]White NJ, Looareesuwan S, Warrell DA, Warrell MJ, Bunnag D, Harinasuta T. Quinine pharmacokinetics and toxicity in cerebral and uncomplicated Falciparum malaria. Am J Med. 1982;73(4):564‐572

[4]Agarwal P, Anvikar AR, Pillai CR, Srivastava K. In vitro susceptibility of Indian Plasmodium falciparum isolates to different antimalarial drugs & antibiotics. Indian J Med Res. 2017;146(5):622‐628

[5]Fuchida S, Yamamoto T, Takiguchi T, Kandaudahewa G, Yuyama N, Hirata Y. Association between underweight and taste sensitivity in middle- to old-aged nursing home residents in Sri Lanka: a cross-sectional study. J Oral Rehabil. 2013;40(11):854‐863