69372-19-6

69372-19-6 structure

Name: pemirolast
Chemical Name: 9-methyl-3-(2H-tetrazol-5-yl)pyrido[1,2-a]pyrimidin-4-one
CAS Number: 69372-19-6
Molecular Formula: C₁₀H₈N₆O
Molecular Weight: 228.21000
Catalog: API Antiallergic Allergic reaction medium blocker
Create Date: 2018-04-11 08:00:00
Modify Date: 2024-01-05 22:42:02
Pemirolast is an orally active antiallergic agent. Pemirolast attenuates paclitaxel hypersensitivity reactions, can be used for bronchial asthma and conjunctivitis research[1]-[5].

Name	9-methyl-3-(2H-tetrazol-5-yl)pyrido[1,2-a]pyrimidin-4-one
Synonyms	3-(1H-tetrazol-5-yl)-9-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidine Pemirolast (INN) UNII-2C09NV773M Pemirox (TN) Pemirolastum [INN-Latin] Pemiroplast Potassium MFCD00864611 Pemirolastum Pemirolast 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one 9-TBX

Description	Pemirolast is an orally active antiallergic agent. Pemirolast attenuates paclitaxel hypersensitivity reactions, can be used for bronchial asthma and conjunctivitis research[1]-[5].
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Inflammation/Immunology
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].
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.
References	[1]. Kawashima T, et al. Inhibitory effect of pemirolast, a novel antiallergic drug, on leukotriene C4 and granule protein release from human eosinophils. Int Arch Allergy Immunol. 1994;103(4):405-9. [2]. Yanni JM, et al. Comparative effects of topical ocular anti-allergy drugs on human conjunctival mast cells. Ann Allergy Asthma Immunol. 1997 Dec;79(6):541-5. [3]. Fujimiya H, et al. Effect of a novel antiallergic drug, pemirolast, on activation of rat peritoneal mast cells: inhibition of exocytotic response and membrane phospholipid turnover. Int Arch Allergy Appl Immunol. 1991;96(1):62-7. [4]. Itoh Y, et al. Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats. Neuropharmacology. 2004 May;46(6):888-94. [5]. Tatsushima Y, et al. Pemirolast reduces cisplatin-induced kaolin intake in rats. Eur J Pharmacol. 2011 Jul 1;661(1-3):57-62.

Density	1.64 g/cm3
Boiling Point	454.8ºC at 760 mmHg
Melting Point	310-311ºC (decomposes)
Molecular Formula	C₁₀H₈N₆O
Molecular Weight	228.21000
Flash Point	228.9ºC
Exact Mass	228.07600
PSA	88.83000
LogP	0.18300

Hazard Codes	C
Risk Phrases	R34:Causes burns.
Safety Phrases	16-26-36/37/39-37/39
RIDADR	UN 1993 3/PG 2
WGK Germany	3
Packaging Group	II
Hazard Class	8

102781-19-1

~74%

69372-19-6

Literature: Wako Pure Chemical Industries, Ltd.; Tokyo, Tanabe Co., Ltd. Patent: US5081243 A1, 1992 ;

132056-88-3

~89%

69372-19-6

Literature: Wako Pure Chemical Industries, Ltd.; Tokyo, Tanabe Co., Ltd. Patent: US5081243 A1, 1992 ;

1603-40-3

122-51-0

109-77-3

69372-19-6

Literature: Sano, Atsunori; Ishihara, Masami Heterocycles, 1998 , vol. 48, # 4 p. 775 - 778

Precursor 4
102781-19-1 1603-40-3 122-51-0 109-77-3
DownStream 1
100299-08-9

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