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/ 组胺受体 / Pemirolast potassium/吡嘧司特钾

Pemirolast potassium/吡嘧司特钾 {[allProObj[0].p_purity_real_show]}

货号：A785978 同义名： BMY 26517; TWT-8152

Pemirolast potassium是一种组胺 H1 受体拮抗剂和肥大细胞稳定剂，具有抗过敏作用。

Pemirolast potassium/吡嘧司特钾 化学结构 CAS号：100299-08-9
Pemirolast potassium/吡嘧司特钾 化学结构
CAS号：100299-08-9
Pemirolast potassium/吡嘧司特钾 3D分子结构
CAS号：100299-08-9
Pemirolast potassium/吡嘧司特钾 化学结构 CAS号：100299-08-9
Pemirolast potassium/吡嘧司特钾 3D分子结构 CAS号：100299-08-9
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Pemirolast potassium/吡嘧司特钾 纯度/质量文件 产品仅供科研

货号：A785978 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 H1 receptor ↓ H2 receptor ↓ H3 receptor ↓ H4 receptor ↓ Histamine receptor ↓ 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine ✔ 97%
Loratadine +

B(0)AT2, IC50: 4 μM

 		98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

 		98%
Doxylamine succinate ✔ 99%
Ebastine ✔ 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

 		98%
Meclizine 2HCl ✔ 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

 		99%
Diphenhydramine HCl ✔ 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

 		++

H2 receptor, pKi: 7.2

 		99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

 		99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

 		98%
Pemirolast potassium ✔ 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

 		98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

 		98%
Brompheniramine maleate ✔ 98%
Carbinoxamine maleate salt ✔ 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

 		98%
Ketotifen fumarate salt ✔ 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

 		PAFR 98%
Famotidine ✔ 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

 		98%
Lafutidine ✔ 99%
Cimetidine ✔ 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

 		AChE 98%
Ranitidine ✔ 96%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		99%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

rat H3 receptor, Ki: 1.44 μM

human H3 receptor, Ki: 1.2 μM

 		98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		99%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 99%
Levodropropizine ✔ 97%
Cyproheptadine HCl ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin HCl ✔ 99+%
Buclizine 2HCl ✔ 95%
Latrepirdine 2HCl ✔ GluR 99%
Cetirizine 2HCl ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Pemirolast potassium/吡嘧司特钾 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].

Pemirolast potassium/吡嘧司特钾 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice Allergic conjunctivitis model Ophthalmic administration 0.1% (w/v) Once daily for 14 days To evaluate the pharmacodynamic effect of Pemirolast Potassium in situ gels on allergic conjunctivitis, the results showed that the in situ gels were highly efficient in suppressing inflammatory symptoms and improving ocular bioavailability. Drug Des Devel Ther. 2021 May 18;15:2099-2107

Pemirolast potassium/吡嘧司特钾 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 - -

Pemirolast potassium/吡嘧司特钾 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

Pemirolast potassium/吡嘧司特钾 实验方案

计算器
存储液制备 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

Pemirolast potassium/吡嘧司特钾 技术信息

CAS号100299-08-9
分子式C10H7KN6O
分子量 266.3
SMILES Code O=C1C(C2=N[N-]N=N2)=CN=C3N1C=CC=C3C.[K+]
MDL No. MFCD01690051
别名 BMY 26517; TWT-8152; TBX; Pemirolast (potassium salt)
运输蓝冰
InChI Key NMMVKSMGBDRONO-UHFFFAOYSA-N
Pubchem ID 443866
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

H2O: 50 mg/mL(187.76 mM)，配合低频超声助溶

配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Pemirolast | 100299-08-9 | TWT-8152 | BMY 26517 | TWT8152 | TWT 8152 | BMY26517 | BMY 26517 | BMY-26517 | Histamine Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Histamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Pemirolast potassium/吡嘧司特钾 纯度/质量文件 | Pemirolast potassium/吡嘧司特钾 亚型比较 | Pemirolast potassium/吡嘧司特钾 生物活性 | Pemirolast potassium/吡嘧司特钾 临床数据 | Pemirolast potassium/吡嘧司特钾 参考文献 | Pemirolast potassium/吡嘧司特钾 实验方案 | Pemirolast potassium/吡嘧司特钾 技术信息

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