专利号:US-10022366-B2 优先权日:2013-04-23 标 题:Extending and maintaining micropore viability of microneedle treated skin with lipid biosynthesis inhibitors for sustained drug delivery 发明人:STINCHCOMB AUDRA L; GHOSH PRIYANKA 权利人:STINCHCOMB AUDRA L; GHOSH PRIYANKA; UNIV MARYLAND; UNIV KENTUCKY RES FOUND 摘要:Microneedles and their use as a physical skin permeation enhancement technique facilitate drug delivery across the skin in therapeutically relevant concentrations. Micropores created in the skin by MNs reseal because of normal healing processes of the skin, thus limiting the duration of the drug delivery window. Pore lifetime enhancement strategies can increase effectiveness of MNs as a drug delivery mechanism by prolonging the delivery window. Fluvastatin (FLU) was used to enhance pore lifetime by inhibiting the synthesis of cholesterol, a major component of the stratum corneum lipids. The skin recovered within a 30-45-min time period following the removal of occlusion, and there was no significant irritation observed due to the treatment compared to the control sites. Thus, it can be concluded that localized skin treatment with FLU can be used to extend micropore lifetime and deliver drugs for up to 7 days across MN-treated skin.
专利号:US-5900227-A 优先权日:1996-06-17 标题 :Multicyclic nitrone spin trapping compositions 发明人:JANZEN EDWARD G; SANKURATRI NAGARAJU 权利人:OKLAHOMA MED RES FOUND 摘要:Multicyclic nitrone spin trapping compounds capable of forming stable free radical spin adducts are provided as well as methods for their synthesis. The multicyclic nitrone spin trapping compounds can be reacted with a free radical, such as a hydroxy or hydroperoxy radical, in solution to form a spin adduct which is stable and readily detectable by electron paramagnetic resonance (EPR) spectroscopy. The multicyclic nitrone spin traps can be used to detect free radicals in a sample such as a biological system. In one embodiment, the spin trapping compound, 1,3,3-trimethyl-6-azabicyclo-[3.2.1]oct-6-ene-N-oxide ('TRAZON') is provided, as well as methods for the synthesis of TRAZON and of modified forms of TRAZON. TRAZON can react with a wide range of different free radicals in solution to form free radical spin adducts which are readily detectable by EPR.
专利号:US-7632519-B2 优先权日:2005-04-25 标 题:TRPV1 agonist compounds, formulations, prodrugs, methods for using the same 发明人:JAMIESON GENE CURTIS; MUHAMMAD NAWEED; BLEY KEITH R 权利人:NEUROGESX INC 摘要:Described here are TRPV1 agonist compounds and their methods of synthesis and use. In addition to specifically identified compounds, capsaicin prodrugs, gemini dimers, and mutual prodrugs are also described. Formulations of the TRPV1 agonist compounds may be in the form of a liquid, tablets, capsules, gel, cream, emulsion, a patch, or the like. Methods for treating medical conditions using the compounds, compositions, or prodrugs described, are also provided.
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 参考文献:10.1007/s11064-008-9752-3 摘要:Mathews JL, Fulton BS, Negus SS, Neumeyer JL, Bidlack JM. In Vivo Characterization of (−)(−)MCL-144 and (+)(−)MCL-193: Isomeric, Bivalent Ligands with Mu/Kappa Agonist Properties. Neurochemical Research. 2008 Jun 05;33(10):2142–50. doi: 10.1007/s11064-008-9752-3.