Anti-allergic properties of ethyl-3-methoxyphenyl-4-thiazolyl-2-oxamate (F 1865).

Abstract

F 1865 (ethyl-3-methoxyphenyl-4-thiazolyl-2-oxamate) has powerful oral anti-allergic properties in immediate hypersensitivity models in rats. In IgE-dependent passive cutaneous anaphylaxis (PCA) the ED50 was of 0.8 mg/kg. In IgG-dependent PCA the ED50 was of 0.6 mg/kg. This oxamate derivative inhibited the liberation of histamine during passive peritoneal anaphylaxis in rats at concentrations of 1 X 10(-6) M or higher. Doses of F 1865, active in PCA, had only weak anti-histamine and anti-serotonin effects, as measured by the increase of cutaneous capillary permeability. Likewise, its inhibitory effect on the bronchospasm due to histamine or serotonin in guinea-pigs was apparent only at doses of 1 mg/kg on i.v. administration. At doses of 100 mg/kg (X2) p.o., F 1865 was inactive against reverse passive Arthus pleurisy induced in rats by rabbit anti-bovine-albumin serum.

• Authors: J P Tarayre, H Lauressergues, F Fauran
• Journal: Archives internationales de pharmacodynamie et de therapie (Arch Int Pharmacodyn Ther) Vol. 260 Issue 1 Pg. 165-76 (Nov 1982) ISSN: 0003-9780 [Print] Belgium
• PMID: 6187305 (Publication Type: Journal Article)

Chemical References

• Amino Acids
• Histamine H1 Antagonists
• Immunoglobulin G
• Serotonin
• Immunoglobulin E
• Histamine
• tioxamast
• Oxamic Acid

Topics

• Amino Acids (pharmacology)
• Animals
• Bronchi (drug effects)
• Capillary Permeability (drug effects)
• Guinea Pigs
• Histamine (pharmacology)
• Histamine H1 Antagonists
• Histamine Release (drug effects)
• Immunoglobulin E (immunology)
• Immunoglobulin G (immunology)
• Male
• Oxamic Acid (analogs & derivatives, pharmacology)
• Passive Cutaneous Anaphylaxis (drug effects)
• Pleurisy (drug therapy)
• Rats
• Rats, Inbred Strains
• Serotonin (pharmacology)