摘要:
The invention relates to the discovery that cis-epoxyeicosatraenoic acids (EETs) bind to and act as agonists of peripheral benzodiazepine receptor and the cannabinoid CB2 receptor. The invention provides methods of reducing symptoms of conditions whose activity is mediated by these receptors, including inhibiting anxiety, inhibiting the growth of cancer cells expressing peripheral benzodiazepine receptors, and reducing oxygen radical damage to cells, by contacting the cells with a cis-epoxyeicosantrienoic acid, an inhibitor of soluble epoxide hydrolase (sEH), or both. The invention further provides methods of inhibiting irritable bowel syndrome by administering to individuals with inhibiting irritable bowel syndrome a cis-epoxyeicosantrienoic acid, an inhibitor of soluble epoxide hydrolase (sEH), or both. In some embodiments, the method comprises administering to the individual a nucleic acid which inhibits expression of sEH.
摘要:
Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
摘要:
Insect pests can be controlled by treating the pests or their loci with a combination of recombinant virus and organic insecticide. The recombinant virus preferably is a baculovirus. Combinations of recombinant baculovirus with chemical insecticides provide a dose-response in pests, such as insects, that is greater than additive. Preferred treatments of the invention are uses of recombinant baculoviruses that express a foreign protein or toxin, with pyrethroid insecticides. Treatments against pyrethroid resistant pests are especially useful.
摘要:
This invention relates to novel haloenol lactone compounds. These compounds have the following general structure: ##STR1## in which Ar is an aryl group and Y is a haloenol lactone moiety. The compounds of the invention are useful for the specific measurement of particular isoenzymes of glutathione S-transferase. Measurement of glutathione S-transferase isoenzymes has importance in diagnostic medicine. The compounds of the invention are also useful for treatment of drug resistance in cancer and for preventing herbicide resistance in plants.
摘要:
A diagnostic or control composition is useful to characterize or control insects and comprises a nucleotide sequence coding for juvenile hormone esterase (JHE). The coding sequence may be combined with a promoter sequence regulating the transcription thereof in a recombinant expression vector for use in controlling insects having a juvenile hormone esterase dependency. Preferred embodiments of the invention are recombinant baculoviruses in which a mutated JHE coding sequence provides relatively rapid speed of kill in insects.
摘要:
The present invention provides compounds and compositions, e.g., a series of compounds wherein a 1,5-biarylpyrazole group is conjugated to a urea group by a non-cleavable covalent chain, that are useful as dual COX-2/sEH inhibitors. The compounds disclosed herein have activity associated with the arachidonate cascade. The activity of these compounds was demonstrated using a lipopolysaccharide (LPS) induced model of pain in the rat. The compounds of the present invention demonstrated superior anti-allodynic activity as compared to the same dose of celecoxib, i.e., a COX-2 inhibitor, also as compared to the same dose of t-AUCB, i.e., a sEH inhibitor, and also as compared to the co-administered same dose of both celecoxib and t-AUCB. The dual inhibitors of the present invention demonstrate enhanced in vivo anti-allodynic activity in a nociceptive behavioral assay. In addition, the compounds of the present invention also demonstrated to have potent anti-angiogenic effects toward endothelial cells (HUVEC) and inhibit angiogenesis in vitro, ex vivo and in vivo. The dual inhibitors of the present invention also demonstrate anti-angiogenic effect to slow breast tumor growth in vivo.
摘要:
Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
摘要:
The invention discloses methods of using cis-epoxyeicosantrienoic acids (“EETs”), inhibitors of soluble epoxide hydrolase (“sEH”), or a combination of an EET and an inhibitor of sEH, to alleviate neuropathic pain in subjects suffering from such pain.