化合物 Pemirolast T60289

Product Introduction
Bioactivity


英文名: Pemirolast

描述: Pemirolast 是一种具有口服活性的抗过敏剂。Pemirolast 通过抑制感觉神经肽的释放来减轻紫杉醇超敏反应，可用于对支气管哮喘和结膜炎的研究。

体外活性: 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 alleviates 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].

体内活性: Pemirolast potently reduces 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途