n-methylsulfonyl-6-(2-propargyloxyphenyl)hexanamide has been researched along with 17-octadecynoic-acid* in 2 studies
2 other study(ies) available for n-methylsulfonyl-6-(2-propargyloxyphenyl)hexanamide and 17-octadecynoic-acid
| Article | Year |
|---|---|
Heme Modification Contributes to the Mechanism-Based Inactivation of Human Cytochrome P450 2J2 by Two Terminal Acetylenic Compounds.
The mechanism-based inactivation of human CYP2J2 by three terminal acetylenic compounds: Topics: Alkynes; Amides; Butyrophenones; Chromatography, Liquid; Cytochrome P-450 CYP2J2; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Danazol; Enzyme Activation; Fatty Acids, Unsaturated; Heme; Humans; Kinetics; Piperidines; Tandem Mass Spectrometry | 2017 |
Selective inhibition of arachidonic acid epoxidation in vivo.
Cytochrome P450 (CYP)-derived arachidonic acid metabolites, including epoxyeicosatrienoic acids (EETS) and 20-HETE, have been implicated in the regulation of renal function and vascular tone. Studying the function of specific CYP arachidonate metabolites has been hampered due to lack of selective inhibitors and difficulty in their solubilization. We have identified MS-PPOH as a potent and selective inhibitor of CYP-catalyzed arachidonate epoxidation in vitro. We used 2-hydroxypropyl-beta-cyclodextrin as a vehicle in order to administer MS-PPOH in vivo. One hour after administration, MS-PPOH (5 mg, IV bolus) significantly inhibited arachidonic acid epoxidation in rat renal cortical microsomes (vehicle-282 +/- 12 pmol/mg/min, MS-PPOH-206 +/- 10 pmol/mg/min, p < 0.05) but had no effect on 20-HETE formation (vehicle-383 32 pmol/mg/min, MS-PPOH-367 +/- 9 pmol/mg/min). The inhibitory effect lasts at least for 6 hours. There was no inhibition of 20-HETE synthesis at any time point. We also examined the effect of MS-PPOH on renal excretiry function. Three hours after MS-PPOH administration to anesthetized rats, urine flow rate became significantly higher (vehicle-275 +/- 16 microl/hour, MS-PPOH-406 +/- 44 microl/hour, p < 0.05). Sodium excretion rate was also significantly higher (vehicle-28.7 +/- 4 micromol/hour, MS-PPOH-63.3 +/- 10 micromol/hour, p < 0.05) but potassium excretion rate was not affected (vehicle-65.5 +/- 5 micromol/hour, MS-PPOH-79.2 +/- 2 micromol/hour). These results suggest that MS-PPOH may be useful as a selective inhibitor of CYP-catalyzed arachidonic acid epoxidation in vivo, and implicate EETs and anti-diuretic and anti-natriuretic in the regulation of renal function. Topics: 8,11,14-Eicosatrienoic Acid; Amides; Animals; Arachidonic Acid; Chromatography, High Pressure Liquid; Cyclodextrins; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Enzyme Inhibitors; Fatty Acids, Unsaturated; Humans; Immunoblotting; Kidney; Male; Miconazole; Microsomes; Organophosphorus Compounds; Rats; Rats, Sprague-Dawley; Recombinant Proteins; Sulfones | 2000 |