Binding of propranolol and iodocyanopindolol to isolated cells, homogenates and plasma membranes of rat liver, lung, kidney and heart.

abstract：:Glyburide is a second-generation sulfonylurea hypoglycemic drug used for the treatment of select women with pregestational and gestational diabetes mellitus (GDM). In vitro and in vivo investigations demonstrated its very low transplacental transfer to the fetal circulation. However, the factors influencing its low tr...

journal_title：Biochemical pharmacology

authors： Nanovskaya TN,Nekhayeva I,Hankins GD,Ahmed MS

更新日期：2006-08-28 00:00:00

abstract：:[[trans-PtCl(NH(3))(2)](2)mu-(trans-Pt(NH(3))(2)(H(2)N(CH(2))(6)-NH(2))(2))](4+) (BBR3464) is a cationic trinuclear platinum drug that is being evaluated in phase II clinical trials for treatment of lung and ovarian cancers. The structure and DNA binding profile of BBR3464 is different from drugs commonly used clinica...

journal_title：Biochemical pharmacology

authors： Kabolizadeh P,Ryan J,Farrell N

更新日期：2007-05-01 00:00:00

abstract：:Aberrant signal transduction by mutant or overexpressed protein kinases has emerged as a promising target for treatment of acute myeloid leukemia (AML). We here present a novel low molecular weight kinase inhibitor, AKN-032, targeting the FMS-like tyrosine kinase 3 (FLT3) and discovered in a new type of screening funn...

journal_title：Biochemical pharmacology

authors： Eriksson A,Höglund M,Lindhagen E,Aleskog A,Hassan SB,Ekholm C,Fhölenhag K,Jensen AJ,Löthgren A,Scobie M,Larsson R,Parrow V

更新日期：2010-11-15 00:00:00

abstract：:We have reported previously that serotonin (5-HT) stimulates the mitogenesis of bovine pulmonary artery smooth muscle cells (SMCs) through active transport of 5-HT and cellular signaling that includes elevation of superoxide (O2.-) and enhancement of protein tyrosine phosphorylation. Ginkgo biloba extract 501 (EGb 501...

journal_title：Biochemical pharmacology

authors： Lee SL,Wang WW,Lanzillo J,Gillis CN,Fanburg BL

更新日期：1998-08-15 00:00:00

abstract：:Treatment of immature 21-day-old female Sprague-Dawley rats with 17 beta-estradiol (E2) (0.5 microgram/rat) caused a significant increase in uterine wet weight, DNA synthesis, progesterone receptor (PR) binding, and peroxidase activity. At doses as high as 40 mg/rat, the bioflavonoid naringenin did not cause a signifi...

journal_title：Biochemical pharmacology

authors： Ruh MF,Zacharewski T,Connor K,Howell J,Chen I,Safe S

更新日期：1995-10-26 00:00:00

abstract：:The effect of glutathione depletion on cytotoxicity of the anthracycline daunorubicin, and of a copper:bis-thiosemicarbazone chelate, was examined in the P388 murine leukemia and its anthracycline-resistant subline, P388/ADR. Depletion of intracellular glutathione was accomplished through exposure to buthionine sulfox...

journal_title：Biochemical pharmacology

authors： Romine MT,Kessel D

更新日期：1986-10-01 00:00:00

abstract：:Retinoic acid isomers have been used with some success as chemotherapeutic agents, most recently with 13-cis retinoic acid showing impressive clinical efficacy in the paediatric malignancy neuroblastoma. The aim of this commentary is to review the evidence that 13-cis retinoic acid is a pro-drug, and consider the impl...

journal_title：Biochemical pharmacology

authors： Armstrong JL,Redfern CP,Veal GJ

更新日期：2005-05-01 00:00:00

abstract：:a synthetic seleno-organic compound, 2-phenyl-1,2-benzoisoselenazol-3(2H)-one (PZ 51), exhibits GSH peroxidase-like activity in vitro, in contrast to its sulfur analog, PZ 25. In addition, PZ 51 behaves as an antioxidant shown by a temporary protection of rat liver microsomes against ascorbate/ADP-Fe-induced lipid per...

journal_title：Biochemical pharmacology

authors： Müller A,Cadenas E,Graf P,Sies H

更新日期：1984-10-15 00:00:00

abstract：:Rat hepatocytes cultured in a sandwich configuration form functional canalicular networks. The influence of extracellular matrix configuration, medium composition, and confluency on the expression and function of Bsep, Mrp2, and Mdr1a/b in sandwich-cultured (SC) rat hepatocytes was examined. Primary rat hepatocytes we...

journal_title：Biochemical pharmacology

authors： Turncliff RZ,Tian X,Brouwer KL

更新日期：2006-05-14 00:00:00

abstract：:Resveratrol decreases basal and induced CYP1A1 mRNA/protein levels in both in vitro and in vivo models, and some studies suggest that resveratrol acts as an aryl hydrocarbon receptor (AhR) antagonist. Treatment of T47D or MCF-7 cells with 10 microM resveratrol inhibited induction of CYP1A1 mRNA and CYP1A1-dependent ac...

journal_title：Biochemical pharmacology

authors： Lee JE,Safe S

更新日期：2001-10-15 00:00:00

abstract：:Cyclosporine A (CsA) is the immunosuppressor most frequently used in transplant surgery and in the treatment of autoimmune diseases because of its specific inhibiting effect on signal transduction pathways of cell T receptor. It has been shown that CsA is able to generate reactive oxygen species and lipid peroxidation...

journal_title：Biochemical pharmacology

authors： Andrés D,Bautista M,Cascales M

更新日期：2005-02-01 00:00:00

abstract：:The neuroprotective effects of adenosine are well-recognized. Recently, propentofylline, a xanthine derivative, has been shown to increase extracellular concentrations of adenosine in ischemic brain and to limit the extent of neuronal damage in experimental models of cerebral ischemia. Since the concentration of adeno...

journal_title：Biochemical pharmacology

authors： Parkinson FE,Paterson AR,Young JD,Cass CE

更新日期：1993-09-01 00:00:00

abstract：:The effect of specifically derivatized dextrans, with or without antiproliferative activity on smooth muscle cells (SMC), was investigated on type I and type III collagen biosynthesis and mRNA levels in post-confluent SMC cultures. Our results indicate that dextran derivatives decreased total protein and collagen synt...

journal_title：Biochemical pharmacology

authors： Benazzoug Y,Logeart D,Labat-Robert J,Robert L,Jozefonvicz J,Kern P

更新日期：1995-03-15 00:00:00

abstract：:Human mono- and lymphocytes from peripheral blood and the monoblastoid cell line U-937 were used in this in vitro study of drug-induced lipidosis. Mono- and lymphocytes were exposed for 4 days to three different tricyclic antidepressants (TCAs), imipramine (25 microM), clomipramine (10 microM) and citalopram (80 micro...

journal_title：Biochemical pharmacology

authors： Xia Z,Appelkvist EL,DePierre JW,Nässberger L

更新日期：1997-05-15 00:00:00

abstract：:Phospholipase A2 activity was detected in 7-day-old carrageenin-induced inflammatory tissue of rats using a synthetic substrate. 1-acyl-2-[3H]arachidonyl-phosphatidylcholine. The inflammatory tissue was homogenized in saline containing 1 M KCl, and the 105,000 g supernatant fraction was placed on a Sephadex G-100 colu...

journal_title：Biochemical pharmacology

authors： Ohuchi K,Watanabe M,Numajiri N,Tsurufuji S

更新日期：1982-09-15 00:00:00

abstract：:Tumor cells proliferate under conditions of oxidative stress. A novel therapeutic approach would be to enhance the cellular effects of the reactive oxygen species formed under these conditions by supplementation with a redox catalyst. This provides a means to target and specifically destroy cancer cells via oxidation ...

journal_title：Biochemical pharmacology

authors： Giles NM,Giles GI,Holley JE,Gutowski NJ,Jacob C

更新日期：2003-11-15 00:00:00

abstract：:Our results indicate that sex hormones play an important role in the regulation of brain and hepatic GST protein during maturity. The conjugating factor GSH does not appear to be under the influence of sex hormones. These observations are of great significance in view of the possibility of continued exposure to neurot...

journal_title：Biochemical pharmacology

authors： Das M,Agarwal AK,Seth PK

更新日期：1982-12-01 00:00:00

abstract：:The effects of 3-monoalkyl- and 3,5-dialkyl-substitution on the cytotoxicity of paracetamol (PAR) in rat hepatocytes was studied. PAR is known to be bioactivated by the hepatic microsomal cytochrome P-450 containing a mixed-function oxidase system presumably to N-acetyl-para-benzoquinone imine (NAPQI), a reactive meta...

journal_title：Biochemical pharmacology

authors： Van De Straat R,De Vries J,Kulkens T,Debets AJ,Vermeulen NP

更新日期：1986-11-01 00:00:00

abstract：:Phentermine was shown in the 1970s to inhibit the metabolism of serotonin by monoamine oxidase (MAO), but never was labeled as an MAO inhibitor; hence, it was widely used in combination with fenfluramine, and continues to be used, in violation of their labels, with other serotonin uptake blockers. We examined the effe...

journal_title：Biochemical pharmacology

authors： Ulus IH,Maher TJ,Wurtman RJ

更新日期：2000-06-15 00:00:00

abstract：:The effects of 2-[(4-acetylphenyl)amino]-3-chloro-1,4-naphthalenedione (NQ-Y15), a synthetic 1,4-naphthoquinone derivative, on platelet activity and its mechanism of action were investigated. NQ-Y15 caused a concentration-dependent inhibition of the aggregation induced by thrombin, collagen, arachidonic acid (AA), and...

journal_title：Biochemical pharmacology

authors： Chang TS,Kim HM,Lee KS,Khil LY,Mar WC,Ryu CK,Moon CK

更新日期：1997-07-15 00:00:00

abstract：:Chronic ethanol use can lead to folic acid deficiency in humans. In rats, acute doses of ethanol produce a marked increase in the urinary excretion of folate which is followed by a decrease in plasma folate levels. To assess the respective roles of ethanol and its metabolism in these effects, five groups of male Sprag...

journal_title：Biochemical pharmacology

authors： McMartin KE,Collins TD

更新日期：1983-09-01 00:00:00

abstract：:1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) is believed to induce neurotoxicity by inhibiting mitochondrial oxidative metabolism, whereas acetyl-L-carnitine (ALC) facilitates this process by transporting fatty acids into mitochondria for beta oxidation. We investigated whether large doses of ALC given by gavag...

journal_title：Biochemical pharmacology

authors： Harik SI,Hritz MA

更新日期：1993-05-25 00:00:00

abstract：:Membranes of neuroblastoma N1E-115 cells contain a specific protein carboxyl methyltransferase that methylates a 70 kD protein and a group of 21-23 kD proteins which are tightly bound to the membranes. The enzyme catalyzes the transfer of [methyl-3H] groups from [methyl-3H]S-adenosyl-L-methionine (Km = 0.22 microM) to...

journal_title：Biochemical pharmacology

authors： Haklai R,Kloog Y

更新日期：1990-09-15 00:00:00

abstract：:A selected number of 1,3-diaminobenzo[f]quinazolines and 1,3-diamino-5,6-dihydrobenzo[f]quinazolines, which may be viewed as tricyclic analogues of the lipid-soluble antifolates pyrimethamine (PM), metoprine (DDMP), and etoprine (DDEP), were tested as inhibitors of purified dihydrofolate reductase (DHFR) from WI-L2 ly...

journal_title：Biochemical pharmacology

authors： Rosowsky A,Freisheim JH,Hynes JB,Queener SF,Bartlett M,Smith JW,Lazarus H,Modest EJ

更新日期：1989-08-15 00:00:00

abstract：:It has been suggested that vasoactive intestinal polypeptide (VIP) has a role as a neurotransmitter and that it participates in the control of hormone release from thyroid follicles. Many hormones and neurotransmitters alter the ionic permeability properties of the plasma membrane of their target cells when they bind ...

journal_title：Biochemical pharmacology

authors： Green ST

更新日期：1987-12-15 00:00:00

abstract：:SR 4233 (3-amino-1,2,4-benzotriazine-1,4-dioxide) is a novel benzotriazine di-N-oxide which shows unusually high selective toxicity towards hypoxic cells, probably as a result of reductive bioactivation. Using an HPLC assay for the parent drug and its 2- and 4-electron reduction products (SR 4317 and SR 4330, respecti...

journal_title：Biochemical pharmacology

authors： Walton MI,Workman P

更新日期：1990-06-01 00:00:00

abstract：:Necroptosis is a form of programmed, caspase-independent cell death that is involved in various pathologic disorders such as ischemia/reperfusion injury, acute kidney injury and inflammatory bowel diseases. Identification of necroptosis inhibitors has great therapeutic potential for the treatment of necroptosis-associ...

journal_title：Biochemical pharmacology

authors： Qin X,Hu L,Shi SN,Chen X,Zhuang C,Zhang W,Jitkaew S,Pang X,Yu J,Tan YX,Wang HY,Cai Z

更新日期：2020-07-01 00:00:00

abstract：:Casein-elicited mouse peritoneal macrophages cultured in the presence of phorbol 12-myristate 13-acetate (PMA) express u-PA. Induction is maximal after 4 hr of stimulation and u-PA activity is mainly recovered with the membrane fraction of the cellular lysate. This enzymatic activity is inhibited by isopropylmethylpho...

journal_title：Biochemical pharmacology

authors： Dubois P,Lison D,Lauwerys R

更新日期：1988-06-01 00:00:00

abstract：:Human flavin-dependent monooxygenase (FMO) isoforms 1 and 3 were expressed by retroviral gene transfer in mouse C3H/10T1/2 cells. FMO function was determined by the sulfoxidation of p-tolylmethylsulfide (TMS). Enzyme activity ranged from 4 to 30 nmol p-tolylmethylsulfoxide (TMSO)/30 min/mg cell protein for FMO 3 clone...

journal_title：Biochemical pharmacology

authors： Smith PB,Crespi C

更新日期：2002-06-01 00:00:00

abstract：:Phosphatidylinositol specific phospholipase C from Staphylococcus aureus could solubilize acetylcholinesterase up to 55% from sheep platelets in the presence of ethylenediaminetetra acetic acid (EDTA). The endogenous phosphatidylinositol specific phospholipase C of platelets activated by deoxycholate (at 3-5 mM) could...

journal_title：Biochemical pharmacology

authors： Majumdar R,Balasubramanian AS

更新日期：1985-12-01 00:00:00