Pharmacological profile of the novel potent antirheumatic 4-(2',4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid
Language English Country Germany Media print
Document type Journal Article
PubMed
9205780
Knihovny.cz E-resources
- MeSH
- Anti-Inflammatory Agents, Non-Steroidal pharmacology therapeutic use toxicity MeSH
- Arthritis, Experimental drug therapy MeSH
- Abdominal Pain chemically induced drug therapy MeSH
- Butyrates pharmacology therapeutic use toxicity MeSH
- Diclofenac therapeutic use MeSH
- Dinoprostone metabolism MeSH
- Edema chemically induced drug therapy MeSH
- Phagocytosis drug effects MeSH
- Phenylbutyrates therapeutic use MeSH
- Carrageenan MeSH
- Rats MeSH
- Arachidonic Acid MeSH
- Acetic Acid MeSH
- Leukotriene B4 metabolism MeSH
- Mice, Inbred C57BL MeSH
- Mice MeSH
- Pleurisy chemically induced drug therapy MeSH
- Rats, Inbred Lew MeSH
- Graft vs Host Reaction drug effects MeSH
- Stomach Ulcer chemically induced MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Male MeSH
- Mice MeSH
- Female MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Anti-Inflammatory Agents, Non-Steroidal MeSH
- Butyrates MeSH
- Diclofenac MeSH
- Dinoprostone MeSH
- fenbufen MeSH Browser
- Phenylbutyrates MeSH
- flobufen MeSH Browser
- Carrageenan MeSH
- Arachidonic Acid MeSH
- Acetic Acid MeSH
- Leukotriene B4 MeSH
On the basis of basic screening for novel, more potent antiarthritics VUFB-16066 (4-(2',4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid, CAS 112344-S2-2) was chosen as a compound with pronounced anti-inflammatory and immunomodulatory effects, with good gastric tolerance and relatively low toxicity. VUFB-16066 is a dual cyclooxygenase and 5-lipoxygenase inhibitor, and it suppresses alloantigen-driven cellular immune response and phagocytosis of stimulated peritoneal cells. VUFB-16066 exhibits prolonged pharmacological activity connected with its major metabolite having a very long half-life. In the model of adjuvant arthritis VUFB-16066 improves most of disease symptoms including immunopathological disturbances, which indicates possible disease-modifying activity of the drug. The beneficial antiarthritic effect of VUFB-16066 has been also confirmed in patients with rheumatoid arthritis.
