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Pemirolast potassium

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Chemical Structure| 100299-08-9 同义名 : BMY 26517;TWT-8152;TBX;Pemirolast (potassium salt)
CAS号 : 100299-08-9
货号 : A785978
分子式 : C10H7KN6O
纯度 : 98%
分子量 : 266.3
MDL号 : MFCD01690051
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 50 mg/mL(187.76 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • H1 receptor
描述 Pemirolast potassium is an antiallergic drug with high safety. Pemirolast potassium 1 and 10 mg/kg markedly inhibited proteinuria in the reversible model. In the irreversible model, pemirolast potassium 3 mg/kg showed a significant decrease in the incidence of glomerulosclerosis. In chronic glomerulonephritis patients, pemirolast potassium, 10 mg twice daily, for 6 months, significantly reduced the severity of proteinuria[3]. Twice-daily administration of pemirolast potassium was as efficacious and safe as twice-daily nedocromil sodium in the 8-week treatment of ragweed allergic conjunctivitis and was superior to nedocromil in comfort[4]. Pemirolast potassium, an antiallergic agent, has preventive effects against restenosis after percutaneous transluminal coronary angioplasty (PTCA)[5]. Levocabastine and pemirolast inhibited histamine release from the rat conjunctiva in correlation with a decrease in histamine content in tears. A potentiating effect induced by the simultaneous use of levocabastine and pemirolast may be attributable to the antihistaminic activity of levocabastine and histamine release inhibition by levocabastine and pemirolast[6]. As an antiallergic drug, pemirolast potassium (TBX) at concentrations between 0.01 and 10 micrograms/ml inhibited antigen (Ag)-stimulated degranulation in RBL-2H3 cells, which have the properties of mucosal mast cells[7].
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
NCT02609334 Asthma Phase 2 Completed - Denmark ... 展开 >> Hvidovre Hospital Hvidovre, Denmark, 2650 Bisbebjerg Hospital København NV, Denmark, 2400 收起 <<
NCT03119714 Allergic Asthma Phase 2 Recruiting April 2018 Sweden ... 展开 >> Lung and Allergy Research Unit C2-88 Karolinska University Hospital Huddinge Recruiting Stockholm, Sweden, 14186 Contact: Barbro Dahlén, MD,PhD    +46858586785    barbro.dahlen@ki.se    Contact: Nikolaos Lazarinis, MD    +46768760476    nikolaos.lazarinis@ki.se 收起 <<
NCT02517372 Healthy Volunteers Phase 1 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.76mL

0.75mL

0.38mL

18.78mL

3.76mL

1.88mL

37.55mL

7.51mL

3.76mL
参考文献

[1]Tatsushima Y, Egashira N, et al. Pemirolast reduces cisplatin-induced kaolin intake in rats. Eur J Pharmacol. 2011 Jul 1;661(1-3):57-62.

[2]Kemp JP, Bernstein IL, et al. Pemirolast, a new oral nonbronchodilator drug for chronic asthma. Ann Allergy. 1992 Jun;68(6):488-91.

[3]Gohda T, Ra C, Hamada C, Tsuge T, Kawachi H, Tomino Y. Suppressive activity of pemirolast potassium, an antiallergic drug, on glomerulonephritis. Studies in glomerulonephritis model rats and in patients with chronic glomerulonephritis concurrently affected by allergic rhinitis. Arzneimittelforschung. 2008;58(1):18-23

[4]Shulman DG. Two mast cell stabilizers, pemirolast potassium 0.1% and nedocromil sodium 2%, in the treatment of seasonal allergic conjunctivitis: a comparative study. Adv Ther. 2003 Jan-Feb;20(1):31-40

[5]Yoshinuma M. [Preventive mechanisms and effects of pemirolast potassium on restenosis after percutaneous transluminal coronary angioplasty: serial coronary angiography and intravascular ultrasound studies]. J Cardiol. 1999 Feb;33(2):81-8. Japanese

[6]Minami K, Hossen MA, Kamei C. Increasing effect by simultaneous use of levocabastine and pemirolast on experimental allergic conjunctivitis in rats. Biol Pharm Bull. 2005 Mar;28(3):473-6

[7]Fujimiya H, Nakashima S, Kumada T, Nakamura Y, Miyata H, Nozawa Y. An antiallergic drug, pemirolast potassium, inhibits inositol 1,4,5-trisphosphate production and Ca2+ mobilization in antigen-stimulated rat basophilic leukemia (RBL-2H3) cells. Arerugi. 1994 Feb;43(2 Pt 1):142-51