Anti-allergic properties of ethyl-3-methoxyphenyl-4-thiazolyl-2-oxamate (F 1865).
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.
D000596:Amino Acids / Q000494:pharmacology*; D000818:Animals; D001980:Bronchi / Q000187:drug effects; D002199:Capillary Permeability / Q000187:drug effects; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D006634:Histamine H1 Antagonists; D006636:Histamine Release / Q000187:drug effects; D007073:Immunoglobulin E / Q000276:immunology; D007074:Immunoglobulin G / Q000276:immunology; D008297:Male; D010072:Oxamic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D010998:Pleurisy / Q000188:drug therapy; D051381:Rats; D011919:Rats, Inbred Strains; D012701:Serotonin / Q000494:pharmacology
D000596:Amino Acids; D006634:Histamine H1 Antagonists; D007074:Immunoglobulin G; D012701:Serotonin; D007073:Immunoglobulin E; D006632:Histamine; C037054:tioxamast; D010072:Oxamic Acid