Drugs online research references
J Pharmacol Exp Ther. 2001 Jan;296(1):188-97.
Stimulatory effect of clofibrate and gemfibrozil administration on the formation of fatty acid esters of estradiol by rat liver microsomes.
Xu S, Zhu BT, Conney AH.
Laboratory for Cancer Research, Department of Chemical Biology, College of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, New Jersey 08854-8020, USA.
Fatty acyl-coenzyme A (CoA):estradiol acyltransferase in liver microsomes catalyzes the formation of estradiol fatty acid esters. These esters are lipophilic and have prolonged hormonal activity because they are slowly metabolized and because they slowly release estradiol. In the present study, we have shown that treatment of rats with clofibrate or gemfibrozil (peroxisome proliferators that are commonly used hypolipidemic drugs) markedly stimulate the liver microsomal esterification of estradiol. Administration of 0.15, 0.30, 0.45, or 0.60% clofibrate in an AIN-76A diet to female rats for 4 weeks stimulated fatty acyl-CoA:estradiol acyltransferase activity per milligram of microsomal protein by 4-, 8-, 14- and 16-fold, respectively, when estradiol was incubated with liver microsomes and a fatty acyl-CoA. Additional studies showed that incubation of (3)H-labeled estradiol with liver microsomes, ATP, and coenzyme A resulted in the formation of multiple fatty acid esters of estradiol from endogenous fatty acids in liver microsomes, and the formation of these esters was stimulated manyfold by pretreatment of rats with clofibrate. This study provides the first demonstration of a stimulatory effect of an environmental agent on the esterification of an estrogen.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11123380&dopt=Abstract
J Steroid Biochem Mol Biol. 1994 Dec;51(5-6):307-13.
Gemfibrozil treatment is associated with elevated adrenal androgen, androstanediol glucuronide and cortisol levels in dyslipidemic men.
Hautanen A, Manttari M, Manninen V, Adlercreutz H.
Department of Clinical Chemistry, University of Helsinki, Finland.
We have investigated the role of steroid hormones as coronary risk factors in the Helsinki Heart Study population of dyslipidemic middle-aged men. We compare here the effects of gemfibrozil and placebo on the serum levels of dehydroepiandrosterone (DHEA), its sulfate (DHEAS), their metabolite androstanediol glucuronide (3 alpha-AdiolG), androstenedione, cortisol, testosterone, and sex-hormone binding globulin (SHBG) in non-smokers. We also examined the associations between steroid and lipoprotein levels in both treatment groups. Compared with placebo gemfibrozil treatment was associated with significant elevations of the mean levels of DHEA 10.2 vs 8.0 nmol/l; P < 0.005, of DHEAS 8.0 vs 5.8 mumol/l; P < 0.001, of 3 alpha AdiolG 18.3 vs 8.4 nmol/l; P < 0.001, of androstenedione 5.7 vs 5.1 nmol/l; P < 0.02, and of cortisol 426 vs 358 nmol/l; P < 0.001. The mean SHBG levels decreased from 46.4 to 41.7 nmol/l; P = 0.03 with gemfibrozil treatment. No difference was found in testosterone levels 17.7 vs 18.8 nmol/l; P = 0.11, or the ratio of testosterone/SHBG 0.45 vs 0.43; P = 0.23. Positive correlations were found between high density lipoprotein-cholesterol and DHEAS (r = 0.267; P < 0.01) and DHEA (r = 0.282; P < 0.01) levels and negative correlations between low density lipoprotein-cholesterol and 3 alpha-AdiolG (r = -0.400; P < 0.001) and cortisol (r = -0.281; P < 0.01) levels in the gemfibrozil group. Our results indicate that gemfibrozil treatment increases the production and turnover of adrenal androgens and cortisol, and suggest that activation of the adrenocortical function and increased metabolism of androgens are related to the improved lipoprotein pattern during gemfibrozil treatment.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7826893&dopt=Abstract
Pharmazie. 2000 Nov;55(11):811-6.
Gemfibrozil ester and amide derivatives--synthesis, spectroscopic characterisation and QSPR.
Lovrek M, Takac MJ, Zorc B, Boneschans B.
Faculty of Pharmacy and Biochemistry, University of Zagreb, Zagreb, Croatia.
The synthesis and spectroscopic characterisation of various gemfibrozil esters 3 and amides 4 are described. In the first step gemfibrozil was reacted with N-1-benzotriazolecarboxylic acid chloride (1) yielding gemfibrozil benzotriazolide (2). Compound 2 readily reacted with alcohols and amines to form the corresponding esters 3 and amides 4, potential prodrugs of the well known hypolipaemic drug gemfibrozil. The quantitative structure property relationship (QSPR) was studied in the series of gemfibrozil esters and amides. The following topological descriptors and physicochemical parameters were used: Wiener number (W), connectivity index (l chi v), relative molecular mass (M(r)), van der Waals volume (Vw) and parameters of lipophilicity (log P and RM).
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11125995&dopt=Abstract
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