BL-5255, a tetrazolylpyrimidinone with potent oral antiallergy activity in animals.

Abstract

BL-5255, 2-(2-n-propoxyphenyl)-5-(5-1 H-tetrazolyl)pyrimidin-4 (3H)-one, effectively inhibited allergic reactions in sensitized rats or guinea pigs when administered by oral or intravenous routes as the water-soluble sodium or ethanolamine monohydrate salts. In the IgE-mediated rat PCA, BL-5255 was 50 times more potent than disodium cromoglycate by intravenous administration. When administered orally in this model, BL-5255 inhibited the PCA reaction by 50% at 0.1 mg/kg. At less than 0.1 mg/kg p.o., the compound protected conscious actively sensitized guinea pigs from aerosolized antigen-induced collapse. In N. brasiliensis-sensitized rats, BL-5255 administered at 0.1--10 mg/kg p.o. inhibited antigen-induced airway constriction in a dose-related manner. BL-5255 is not a histamine or serotonin antagonist but appears to exert its antiallergic effect by inhibiting the release of mediators.

• Authors: P Siminoff, F C Reed 3rd, J E Schurig, P F Juby
• Journal: Monographs in allergy (Monogr Allergy) Vol. 14 Pg. 318-23 ( 1979) ISSN: 0077-0760 [Print] Switzerland
• PMID: 91959 (Publication Type: Journal Article)

Chemical References

• Azoles
• Histamine H1 Antagonists
• Pyrimidinones
• Tetrazoles
• BL 5255

Topics

• Administration, Oral
• Airway Obstruction (drug therapy)
• Animals
• Azoles (therapeutic use)
• Dose-Response Relationship, Drug
• Guinea Pigs
• Histamine H1 Antagonists
• Histamine Release (drug effects)
• Hypersensitivity (drug therapy)
• Hypersensitivity, Immediate (immunology)
• Male
• Passive Cutaneous Anaphylaxis
• Pyrimidinones (therapeutic use)
• Rats
• Tetrazoles (therapeutic use)