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编 号：F428651
分子式：C10H8N6O
分子量：228.21
分子式：C10H8N6O
分子量：228.21
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CAS No: 69372-19-6
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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-.
体内研究：
Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats.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.).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.).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.Animal Model:Male Wistar rats (6-week-old, 160-250 g)
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)
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.
体外研究：
Pemirolast (1 μM-1 mM) inhibits A23187-induced LTC4 and ECP release from the eosinophils in a dose-dependent manner. Pemirolast (0.1 mM and 1 mM) also inhibits PAF-induced and FMLP-induced ECP release from the eosinophils.Pemirolast prevents the activation of human eosinophils to inhibit granule protein LTQ and ECP release, so that alleviates controlling allergic diseases.Pemirolast (100 nM-1 mM; 1-15 min) fails to significantly inhibit histamine release from human conjunctival mast cells.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 phosphatidylicacid.
Pemirolast is an orally active antiallergic agent. Pemirolast attenuates paclitaxel hypersensitivity reactions, can be used for bronchial asthma and conjunctivitis research-.
体内研究：
Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats.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.).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.).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.Animal Model:Male Wistar rats (6-week-old, 160-250 g)
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)
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.
体外研究：
Pemirolast (1 μM-1 mM) inhibits A23187-induced LTC4 and ECP release from the eosinophils in a dose-dependent manner. Pemirolast (0.1 mM and 1 mM) also inhibits PAF-induced and FMLP-induced ECP release from the eosinophils.Pemirolast prevents the activation of human eosinophils to inhibit granule protein LTQ and ECP release, so that alleviates controlling allergic diseases.Pemirolast (100 nM-1 mM; 1-15 min) fails to significantly inhibit histamine release from human conjunctival mast cells.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 phosphatidylicacid.
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