Biotransformation of 17 beta-hydroxy-11 beta-(4-dimethylaminophenyl)17 alpha-1-propynyl-estra-4,9-dien-3-one (RU486) in rat hepatoma variants.

abstract：:Previous reports have demonstrated that cadmium (Cd) may induce cell death via apoptosis, but the mechanism responsible for cellular death is not clear. In this study, we investigated the signaling pathways implicated in Cd-induced apoptosis in lung epithelial fibroblast (WI 38) cells. Apoptotic features were observed...

journal_title：Biochemical pharmacology

authors： Oh SH,Lee BH,Lim SC

更新日期：2004-11-01 00:00:00

abstract：:The stereoselective sulfoxidation of the pharmacologically active metabolite of sulindac, sulindac sulfide, was characterized in human liver, kidney, and cDNA-expressed enzymes. Kinetic parameter estimates (pH = 7.4) for sulindac sulfoxide formation in human liver microsomes (N = 4) for R- and S-sulindac sulfoxide wer...

journal_title：Biochemical pharmacology

authors： Hamman MA,Haehner-Daniels BD,Wrighton SA,Rettie AE,Hall SD

更新日期：2000-07-01 00:00:00

abstract：:In model experiments using human erythrocytes, glycochenodeoxycholate caused extensive membrane damage (as judged by release of membrane phospholipid and acetylcholinesterase and by cell lysis) at approximately 10-fold lower concentrations than glycocholate. Chenodeoxycholate feeding had no effect upon the total prote...

journal_title：Biochemical pharmacology

authors： Rahman K,Billington D

更新日期：1984-07-15 00:00:00

abstract：:(R,E)-N-(3-(2-acetamido-3-(benzyloxy) propanamido)propyl)-2-cyano-3-(4-hydroxy phenyl)acrylamide (hr5F) was design-synthesized based on bioactivity focus strategy as a potential agent to treat diabetic complicates. With in vitro enzyme assay, it is confirmed that hr5F is an effective ALR2 inhibitor with IC50 value of ...

journal_title：Biochemical pharmacology

authors： Wang Z,Yuan S,Li Y,Zhang Z,Xiao W,Tang D,Ye K,Liu Z,Wang C,Zheng Y,Nie H,Chen H

更新日期：2018-04-01 00:00:00

abstract：:Stimulation of hepatic glycogenolysis and vasoconstriction of the hepatic vasculature in response to acetyl glyceryl ether phosphocholine (AGEPC; platelet activating factor) was inhibited by two structural analogues of AGEPC, U66985 (1-O-octadecyl-2-O-acetyl-sn-glycero-3-phosphoric acid-6'-trimethyl ammonium hexyl est...

journal_title：Biochemical pharmacology

authors： Buxton DB,Hanahan DJ,Olson MS

更新日期：1986-03-15 00:00:00

abstract：:Calcipotriol (MC 903) is a novel analogue of the physiologically active metabolite of vitamin D3, 1 alpha,25-dihydroxycholecalciferol [1,25(OH)2D3]. MC 903 and 1,25(OH)2D3 have similar effects on cell proliferation and cell differentiation in vitro using the human histiocytic lymphoma cell line U 937, but in vivo MC90...

journal_title：Biochemical pharmacology

authors： Kissmeyer AM,Binderup L

更新日期：1991-06-01 00:00:00

abstract：:The mechanisms of toxicity and sensitization by the radiosensitizer misonidazole [1-(2-nitro-1-imidazolyl)-3-methoxy-2-propanol] are not well understood. We report here on the inhibition of total glutathione peroxidase (GSHPx), selenium-dependent glutathione peroxidase (selenium-GSHPx) and glutathione transferase (GSH...

journal_title：Biochemical pharmacology

authors： Kumar KS,Weiss JF

更新日期：1986-09-15 00:00:00

abstract：:This study demonstrates that the exposure of phenobarbitone-treated rats to halothane at an oxygen concentration of either 10% or 14% results in marked decreases in cytochrome P-450 content and aminopyrine demethylase activity in animals sacrificed from 1 to 48 hr post-exposure. The alterations observed in the hepatic...

journal_title：Biochemical pharmacology

authors： Knights KM,Gourlay GK,Cousins MJ

更新日期：1987-03-15 00:00:00

abstract：:We investigated the effects of tranilast on inducible cyclooxygenase (COX2)-mediated prostaglandin E2 (PGE2) production and enzyme induction in interleukin-lbeta (IL-1beta)-stimulated cultured dermal fibroblasts. IL-1beta enhanced PGE2 production in cultured fibroblasts. Tranilast did not affect constitutive cyclooxyg...

journal_title：Biochemical pharmacology

authors： Inoue H,Ohshima H,Kono H,Yamanaka M,Kubota T,Aihara M,Hiroi T,Yago N,Ishida H

更新日期：1997-06-15 00:00:00

abstract：:L-Carnitine is a key molecule in the transfer of fatty acid across mitochondrial membranes. Bioavailable L-carnitine is either provided by an endogeneous biosynthesis or after intestinal absorption of dietary items containing L-carnitine. After intestinal absorption or hepatic biosynthesis, L-carnitine is transferred ...

journal_title：Biochemical pharmacology

authors： Georges B,Galland S,Rigault C,Le Borgne F,Demarquoy J

更新日期：2003-05-01 00:00:00

abstract：:MOLT-4 (T-), RAJI (B-), and KM-3 (non-B-non-T-, common ALL) malignant lymphoblasts demonstrated significant differences in their activities of purine de novo synthesis (PDNS) and purine salvage pathway and in their cell-kinetic parameters. Incubations with concentrations of methotrexate (0.02 and 0.2 microM), which ca...

journal_title：Biochemical pharmacology

authors： Bökkerink JP,De Abreu RA,Bakker MA,Hulscher TW,van Baal JM,Schretlen ED,De Bruijn CH

更新日期：1988-06-15 00:00:00

abstract：:Epothilones constitute a novel class of antitubulin agents that are active in patients who relapse after treatment with other chemotherapeutics. This study investigated the molecular mechanisms leading to the onset of epothilone-B (patupilone) resistance in ovarian cancer. Results demonstrated that the Gli family of t...

journal_title：Biochemical pharmacology

authors： Mozzetti S,Martinelli E,Raspaglio G,Prislei S,De Donato M,Filippetti F,Shahabi S,Scambia G,Ferlini C

更新日期：2012-12-01 00:00:00

abstract：:The effect of the cationic dye, ruthenium red (RR), on ionic fluxes, Ca2+ signal generation, and stimulation of aldosterone production was studied in isolated rat adrenal glomerulosa cells. In these cells, increased extracellular [K+] as well as angiotensin II (Ang II) elevate cytoplasmic Ca2+ concentration and thereu...

journal_title：Biochemical pharmacology

authors： Szabadkai G,Várnai P,Enyedi P

更新日期：1999-01-15 00:00:00

abstract：:The development of neuroprotective agents is necessary for the treatment of neurodegenerative diseases. Here, we report PQA-11, a prenylated quinolinecarboxylic acid (PQA) derivative, as a potent neuroprotectant. PQA-11 inhibits glutamate-induced cell death and caspase-3 activation in hippocampal cultures, as well as ...

journal_title：Biochemical pharmacology

authors： Ogura M,Kikuchi H,Shakespear N,Suzuki T,Yamaki J,Homma MK,Oshima Y,Homma Y

更新日期：2019-04-01 00:00:00

abstract：:Increasing evidence is accumulating that zoledronic acid (ZOL), a nitrogen-containing bisphosphonate (N-BP), is able to affect tumor cells by inhibiting the enzyme farnesyl pyrophosphate synthase (FPPS) in the mevalonate pathway (MVP). The consequent accumulation of unprenylated proteins is believed to largely account...

journal_title：Biochemical pharmacology

authors： Räikkönen J,Mönkkönen H,Auriola S,Mönkkönen J

更新日期：2010-03-01 00:00:00

abstract：:After rats were injected with the reduced glutathione (GSH) depletor phorone (diisopropylidene acetone, 250 mg/kg, i.p.), there was a significant increase in microsomal glutathione S-transferase activity in the liver. The maximum activity was observed 24 hr after injection and was about 2-fold that of the control acti...

journal_title：Biochemical pharmacology

authors： Masukawa T,Iwata H

更新日期：1986-02-01 00:00:00

abstract：:The transient receptor potential vanilloid-4 (TRPV4) belongs to a family of ion channels and can be activated by warm temperature, hypotonicity, cell swelling or lipid mediators of the arachidonic cascade. The metabolites or events responsible for TRPV4 activation are associated with inflammation, arguing in favor of ...

journal_title：Biochemical pharmacology

authors： Vergnolle N

更新日期：2014-05-15 00:00:00

abstract：:A new analogue of methotrexate was synthesized from 4-amino-4-deoxy-N10-methylpteroic acid and D,L-homocysteic acid. The product (mAPA-HCysA) was bound tightly to L1210 mouse leukemia dihydrofolate reductase (IC50 = 1 nM), inhibited L1210 cell proliferation in culture (IC50 = 0.3 microM), and prolonged the survival of...

journal_title：Biochemical pharmacology

authors： Rosowsky A,Moran RG,Forsch R,Colman P,Uren J,Wick M

更新日期：1984-01-01 00:00:00

abstract：:A comparison between the effects of schisandrin B (Sch B) and butylated hydroxytoluene (BHT) treatments on hepatic antioxidant status was made to identify the critical antioxidant action of Sch B involved in hepatoprotection in mice. Whereas Sch B treatment (3 mmol/kg/day x 3, p.o.) increased the hepatic mitochondrial...

journal_title：Biochemical pharmacology

authors： Ip SP,Ko KM

更新日期：1996-12-13 00:00:00

abstract：:This study was designed to examine the relationship between the extent of Sandimmun (cyclosporin A, SIM) metabolism and SIM-induced hepatotoxicity both in vivo and in primary cultures of rat hepatocytes. Firstly, SIM (50 mg/kg p.o.) was administered daily to male Wistar rats for 10 days with or without co-administrati...

journal_title：Biochemical pharmacology

authors： Bouis P,Brouillard JF,Fischer V,Donatsch P,Boelsterli UA

更新日期：1990-01-15 00:00:00

abstract：:Histamine H-1 receptors in human peripheral lung were characterized by radioligand and biochemical assays employing binding of the H-1 receptor antagonist [3H]pyrilamine to plasma membrane preparations. Simultaneous computerized analyses of the data from fourteen separate equilibrium-binding assays indicated the prese...

journal_title：Biochemical pharmacology

authors： Casale TB,Rodbard D,Kaliner M

更新日期：1985-09-15 00:00:00

abstract：:Benzoporphyrin derivative, monoacid ring A (BPD-MA), currently in clinical trials as a photosensitizer for photodynamic therapy for cancer, consists of two regioisomers (A1 and A2) present in equal proportions. The contribution of the regioisomers to the overall photosensitizing potency of BPD-MA was tested in vitro a...

journal_title：Biochemical pharmacology

authors： Richter AM,Jain AK,Canaan AJ,Waterfield E,Sternberg ED,Levy JG

更新日期：1992-06-09 00:00:00

abstract：:In the present study, a screen of adenosine analogs as potential modulators of arylamine-N-acetyltransferase 1 activity identified ATP as an inhibitor within its range of physiological concentrations. Kinetically, ATP was a non-competitive inhibitor with respect to the acetyl acceptor but a competitive inhibitor with ...

journal_title：Biochemical pharmacology

authors： Minchin RF,Rosengren KJ,Burow R,Butcher NJ

更新日期：2018-12-01 00:00:00

abstract：:A newly-synthesized derivative of prazosin, prazosinamine hydrochloride, was examined for its ability to antagonize the interaction of the alpha 1-adrenergic agonist phenylephrine with liver cells. Using a Ca2--selective electrode to measure changes in perfusate Ca2+ concentration, prazosinamine was found to be as eff...

journal_title：Biochemical pharmacology

authors： Armarego WL,Altin JG,Weir RC,Bygrave FL

更新日期：1987-05-15 00:00:00

abstract：:The differentiation-inducing factor-1 (DIF-1) is a lipophilic signal molecule (chlorinated alkylphenone) that induces stalk-cell differentiation in the cellular slime mould Dictyostelium discoideum. It has also been shown that DIF-1 and its derivative (DIF-3) suppress cell growth in mammalian tumor cells. In the prese...

journal_title：Biochemical pharmacology

authors： Gokan N,Kikuchi H,Nakamura K,Oshima Y,Hosaka K,Kubohara Y

更新日期：2005-09-01 00:00:00

abstract：:Folate-binding protein (FBP), a high-affinity folate receptor, is responsible for cellular accumulation of folate and folate analogs such as methotrexate in human KB (nasopharyngeal carcinoma) cells. Both FBP and FBP mRNA increase 3- to 5-fold when KB cells are grown in folate-deficient (less than 10 nM folate) medium...

journal_title：Biochemical pharmacology

authors： Hsueh CT,Dolnick BJ

更新日期：1993-06-22 00:00:00

abstract：:3-Morpholino-sydnonimine (SIN-1) is a NO-releasing compound which mimics the effects of cGMP through activation of soluble guanylyl cyclase. Its prodrug, molsidomine (SIN-10), does not release NO but does modulate various cell functions. These findings prompted us to study the effects of SIN-10 and SIN-1 on the respir...

journal_title：Biochemical pharmacology

authors： Ervens J,Seifert R

更新日期：1992-08-18 00:00:00

abstract：:The dissociation constant (Kd) for the binding of epinephrine to beta-adrenergic receptors of the S49 cell is 2 microM, which is the ratio of the rate constants for dissociation (koff) and association (kon), Kd = koff/kon. Although the Kd is known by direct measurement, the individual rate constants kon and koff are u...

journal_title：Biochemical pharmacology

authors： Stickle D,Barber R

更新日期：1991-08-08 00:00:00

abstract：:The mechanisms by which amiloride and 4,4'-diisothiocyano-2,2'-disulfonic stilbene (DIDS) inhibit hepatic uptake of cholate and taurocholate (TC) were investigated in isolated rat hepatocytes. Amiloride inhibited Na(+)-dependent uptake of cholate and TC only when hepatocytes were preincubated with amiloride, indicatin...

journal_title：Biochemical pharmacology

authors： Anwer MS,Branson AU,Atkinson JM

更新日期：1991-12-11 00:00:00

abstract：:We examined whether any changes were induced in cellular proteins by an inhibitor of acylpeptide hydrolase (ACPH) (EC 3.4.19.1), acetylleucine chloromethyl ketone (ALCK), which was shown in our previous report to induce apoptosis of human U937 cells. Extract prepared from U937 cells in 0.05% Triton X-100-PBS was incub...

journal_title：Biochemical pharmacology

authors： Yamaguchi M,Tsuchiya Y,Chikuma T,Hojo H

更新日期：2002-05-15 00:00:00