Corpus ID: 42957616

Novel, selective delta6 or delta5 fatty acid desaturase inhibitors as antiinflammatory agents in mice.

  title={Novel, selective delta6 or delta5 fatty acid desaturase inhibitors as antiinflammatory agents in mice.},
  author={Mark Gerard Obukowicz and Dean J. Welsch and William J. Salsgiver and Cynthia L. Martin-Berger and Kevin S Chinn and Kevin L. Duffin and Amiram Raz and Philip Needleman},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={287 1},
Decreased synthesis of arachidonic acid by inhibition of the Delta6 or Delta5 desaturase was evaluated as a means to mitigate inflammation. Using quantitative in vitro and in vivo radioassays, novel compounds representing five classes of Delta5 desaturase inhibitors and one class of Delta6 desaturase inhibitor were identified. The Delta6 desaturase inhibitor, SC-26196, had pharmacokinetic and pharmacodynamic profiles in mice that allowed for the evaluation of the pharmacological effects of… Expand
Elevated Delta-6 desaturase (FADS2) gene expression in the prefrontal cortex of patients with bipolar disorder.
It is demonstrated that FADS2 mRNA expression is significantly and selectively elevated in the prefrontal cortex of BD patients, and may contribute to dysregulated central PUFA biosynthesis and pro-inflammatory signaling implicated in the pathophysiology of BD. Expand
Inhibition of delta-6 desaturase reverses cardiolipin remodeling and prevents contractile dysfunction in the aged mouse heart without altering mitochondrial respiratory function.
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Elevated delta-6 desaturase (FADS2) expression in the postmortem prefrontal cortex of schizophrenic patients: Relationship with fatty acid composition
Although emerging evidence suggests that schizophrenia (SZ) is associated with peripheral and central polyunsaturated fatty acid (PUFA) deficits, there is currently nothing known about the expressionExpand
Differential effects of antipsychotic medications on polyunsaturated fatty acid biosynthesis in rats: Relationship with liver delta6-desaturase expression
In vivo data demonstrate that augmentation of PUFA biosynthesis is not common to all antipsychotic medications, and that risperidone and paliperidone uniquely increase delta-6 desaturase (Fads2) mRNA expression and most robustly increase PU FA biosynthesis and peripheral membrane composition. Expand
Omega-3 fatty acid deficiency selectively up-regulates delta6-desaturase expression and activity indices in rat liver: prevention by normalization of omega-3 fatty acid status.
Findings confirm previous findings that liver, but not brain, delta6-desaturase expression and activity indices are negatively regulated by dietary n-3 fatty acids. Expand
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Liver TAG Transiently Decreases While PL n-3 and n-6 Fatty Acids are Persistently Elevated in Insulin Resistant Mice
The data indicate that the early phase of HFD-induced insulin resistance is not associated with elevated liver lipid concentration and the early and persistent rise of arachidonate and docosahexaenoate indicates that insulin Resistance is not due to insufficient availability (or concentrations) of polyunsaturated fatty acids as postulated previously. Expand
Analgesic and anti-inflammatory activities of certain 6-aryl-9-substituted-6,9-diazaspiro-[4,5]decane-8,10-diones in mice
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