Pemirolast 是一种具有口服活性的抗过敏试剂。Pemirolast 能够减轻紫杉醇处理导致的生物过敏反应，可用于对支气管哮喘和结膜炎的研究。
| 生物活性 | Pemirolast is an orally active antiallergic agent. Pemirolast attenuates paclitaxel hypersensitivity reactions, can be used for bronchial asthma and conjunctivitis research[1]-[5]. |
体外研究
(In Vitro) | Pemirolast (1 μM-1 mM) inhibits A23187-induced LTC4 and ECP release from the eosinophils in a dose-dependent manner[1].
Pemirolast (0.1 mM and 1 mM) also inhibits PAF-induced and FMLP-induced ECP release from the eosinophils[1].
Pemirolast prevents the activation of human eosinophils to inhibit granule protein LTQ and ECP release, so that alleviates controlling allergic diseases[1].
Pemirolast (100 nM-1 mM; 1-15 min) fails to significantly inhibit histamine release from human conjunctival mast cells[2].
Pemirolast (0.1 μg/mL-0.01 mg/mL) inhibits the activation of signal transduction phospholipases C and AZ in rat peritoneal mast cells, by inhibiting the degranulation reaction of antigen and compound 48/80, suppressing the formation of 1,2-diacylglycerol and phosphatidylic acid[3].
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体内研究
(In Vivo) | Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats[4].
Pemirolast (0.1-1 mg/kg; i.v.) inhibits taxel-induced pulmonary vascular hyperpermeability, and reverses paclitaxel-induced arterial PaO2 decreasing at a dosage of 1 mg/kg, 30 minutes after paclitaxel injection (15 mg/kg; i.v.)[4].
Pemirolast (1 mg/kg; i.v.) reverses taxel-induced elevation of the concentrations of sensory neuropeptides (CGRP, substance P and neurokinin A), 30 minutes after paclitaxel injection (15 mg/kg; i.v.)[4].
Pemirolast (10 mg/kg/d; p.o.; 4-5 d) significantly reduces cisplatin-induced kaolin intake on days 3 and 4 and inhibits cisplatin-induced substance P release in the cerebrospinal fluid (CSF) in rats[5].
| Animal Model: | Male Wistar rats (6-week-old, 160-250 g)[5] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage; 5 days: 1 h or 30 min before and 24, 48, 72 and 96 h (five times in total) after administration of cisplatin (2-10 mg/kg; i.v.) | | Result: | Inhibited the cisplatin-induced increase in kaolin intake on days 3 and 4, without decreasing in normal feed intake. |
| Animal Model: | Male Wistar rats (6-week-old, 160-250 g)[5] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage; 4 days: 30 min before and 24, 48, 72 and 96 h (four times in total) after administration of cisplatin (5 mg/kg; i.v.). | | Result: | Significantly reversed the cisplatin-induced increase of substance P levels to vehicle levels in the CSF. |
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| Clinical Trial | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(438.19 mM;Need ultrasonic) DMF :< 1 mg/mL (ultrasonic)(insoluble) 配制储备液 | 1 mM | 4.3819 mL | 21.9096 mL | 43.8193 mL | | 5 mM | 0.8764 mL | 4.3819 mL | 8.7639 mL | | 10 mM | 0.4382 mL | 2.1910 mL | 4.3819 mL |
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