abstract：:The formation of triacylglycerols containing fenoprofen was studied in rat isolated adipocytes and hepatocytes incubated with [3H]glycerol and R or S fenoprofen. In both hepatocytes and adipocytes there was a high-affinity enzymatic process for the synthesis of triacylglycerol containing fenoprofen which was stereospe...

journal_title：Biochemical pharmacology

authors： Sallustio BC,Meffin PJ,Knights KM

更新日期：1988-05-15 00:00:00

abstract：:Accumulation of radioactive iron (59Fe) into isolated fragments of rat small intestine in the presence of two hydroxypyrones, maltol and ethyl maltol, was compared with that in the presence of another chelator of iron(III), nitrilotriacetic acid (NTA). The characteristics of uptake were similar with all three ligands....

journal_title：Biochemical pharmacology

authors： Levey JA,Barrand MA,Callingham BA,Hider RC

更新日期：1988-05-15 00:00:00

abstract：:The inhibition of renal ornithine decarboxylase (ODC) by aminoglycoside antibiotics was characterized in the postmitochondrial fraction of a kidney homogenate from adult pigmented guinea pigs. Enzymatic activity was defined as the rate of decarboxylation of [14C]ornithine sensitive to a specific ODC inhibitor, alpha-d...

journal_title：Biochemical pharmacology

authors： Henley CM 3rd,Mahran LG,Schacht J

更新日期：1988-05-01 00:00:00

abstract：:The salt-induced condensation of chromatin has been studied with flow-linear dichroism technique using an intercalative dye (methylene blue) to selectively monitor the linker orientation. At low ionic strength both linkers and chromatosomes (with their flat faces) are oriented preferentially parallel to the chromatin ...

journal_title：Biochemical pharmacology

authors： Kubista M,Nielsen PE,Nordén B

更新日期：1988-05-01 00:00:00

abstract：:Nitrogen dioxide (NO2), an environmental oxidant pollutant, is known to peroxidize membrane lipids of lung cells. We evaluated the ability of NO2 to alter the surface membrane fluidity, lipid composition, and insulin receptor binding of porcine pulmonary artery endothelial cells in culture. After 3- to 24-hr exposure ...

journal_title：Biochemical pharmacology

authors： Patel JM,Edwards DA,Block ER,Raizada MK

更新日期：1988-04-15 00:00:00

abstract：:A marked inhibition of the growth of solid tumor adenocarcinoma 755 was achieved by the combination of 5-fluorouracil (5-FU) with bromovinyldeoxyuridine (BVDU). The therapeutic index (LD50/ED50) for the combination of BVDU plus 5-FU was 8.1 and 3.9 upon intraperitoneal (i.p.) or oral (p.o.) administration, respectivel...

journal_title：Biochemical pharmacology

authors： Iigo M,Araki E,Nakajima Y,Hoshi A,De Clercq E

更新日期：1988-04-15 00:00:00

abstract：:We have investigated the effects of fatty acids on the Na+-H+ exchanger and other carrier-mediated transport systems in intestinal brush-border membrane vesicles. The Na+-H+ exchanger (i.e. H+ gradient-dependent, dimethylamiloride-sensitive Na+ uptake) was strongly inhibited by fatty acids and the inhibition was conce...

journal_title：Biochemical pharmacology

authors： Tiruppathi C,Miyamoto Y,Ganapathy V,Leibach FH

更新日期：1988-04-01 00:00:00

abstract：:Lipoxygenase products, which are formed in great amounts in platelets during their activation, have been prepared from arachidonic acid (20:4n-6), the main polyunsaturated fatty acid (PUFA) esterified in platelet phospholipids, and from two major PUFAs of fish fat, eicosapentaenoic (20:5n-3) and docosahexaenoic (22:6n...

journal_title：Biochemical pharmacology

authors： Croset M,Sala A,Folco G,Lagarde M

更新日期：1988-04-01 00:00:00

abstract：:The present study was designed to investigate the effect of hepatic glutathione depletion induced by intraperitoneal administration of diethyl maleate (DEM) on the maximum biliary transport (Tm) and on the biliary excretion of bromosulfophthalein (BSP) in anaesthetized rabbits when the dye was perfused endovenously at...

journal_title：Biochemical pharmacology

authors： Jiménez R,Larrubia O,Monte MJ,Esteller A

更新日期：1988-04-01 00:00:00

abstract：:Opiates act through a specific receptor to inhibit the striatal adenylate cyclase [ATP pyrophosphate-lyase (cyclizing), EC 4,6.1.1] and stimulate a high-affinity GTPase (EC 3.6.1). The present study analyzes the functions of the striatal adenylate cyclase complex following chronic morphine treatment in the rat. The in...

journal_title：Biochemical pharmacology

authors： Tirone F,Viganó A,Groppetti A,Parenti M

更新日期：1988-03-15 00:00:00

abstract：:We examined the effects of the divalent cation calcium (Ca2+) and the monovalent cations potassium (K+) and sodium (Na+) and different modalities that affect the fluxes of these cations on immunoreactive secretin (IRS) secretion from canine duodenal mucosa in vitro. In the absence of extracellular Ca2+, the basal IRS ...

journal_title：Biochemical pharmacology

authors： Murthy SN,Lavy A

更新日期：1988-03-15 00:00:00

abstract：:The in vivo actions of two antimetabolites, acivicin (NSC-163501) and tiazofurin (NSC-286193), were examined on the enzymic programs of rat bone marrow. From the bone marrow of the femurs, 100,000 g supernatant fractions were prepared; enzymic activities were measured by isotopic assays, and cellularity was determined...

journal_title：Biochemical pharmacology

authors： Prajda N,Natsumeda Y,Ikegami T,Reardon MA,Szondy S,Hashimoto Y,Emrani J,Weber G

更新日期：1988-03-01 00:00:00

abstract：:Dinucleotides of adenosine and thymidine in the ApnT series (n = 3,4,5 and 6) and their corresponding phosphonate analogues, where a methylene group replaces the oxygen between the alpha and beta phosphorus atoms adjacent to thymidine, have been evaluated as inhibitors of human leukaemic thymidylate kinase (dTMP kinas...

journal_title：Biochemical pharmacology

authors： Orr RM,Davies LC,Stock JA,Taylor GA,Powles RL,Harrap KR

更新日期：1988-02-15 00:00:00

abstract：:Daily subcutaneous administration of the oral hypoglycaemic agent, diphenyleneiodonium at a low dose (1.5 mg/kg body weight) over a 4-5 week period resulted in a normoglycaemic stable animal model of impaired oxidative phosphorylation in the rat. Diphenyleneiodonium specifically inhibits NAD-linked mitochondrial oxida...

journal_title：Biochemical pharmacology

authors： Cooper JM,Petty RK,Hayes DJ,Morgan-Hughes JA,Clark JB

更新日期：1988-02-15 00:00:00

abstract：:The subcellular localization of a binding site for the competitive thromboxane A2/prostaglandin H2 (TXA2/PGH2) antagonist, 9,11-dimethylmethano-11,12-methano-16-(3-iodo-4- hydroxyphenyl)-13,14-dihydro-13-aza-15 alpha beta-omega-tetranor TXA2 ([125I]-PTA-OH), was determined. Subcellular fractions of platelets were prep...

journal_title：Biochemical pharmacology

authors： Saussy DL Jr,Mais DE,Baron DA,Pepkowitz SH,Halushka PV

更新日期：1988-02-15 00:00:00

abstract：:Uteroglobin, a steroid-dependent secretory protein first discovered in the rabbit uterus during early pregnancy, is a potent phospholipase A2 inhibitor. We found that uteroglobin also inhibited human and rabbit phagocyte chemotaxis in response to formyl peptide attractants in a dose-dependent manner. Half-maximal inhi...

journal_title：Biochemical pharmacology

authors： Vasanthakumar G,Manjunath R,Mukherjee AB,Warabi H,Schiffmann E

更新日期：1988-02-01 00:00:00

abstract：:The normal sexual dimorphism in murine hepatic hexobarbital metabolism (i.e. females greater than males) was found to be absent in senescent animals. Hexobarbital metabolism, expressed as microsomal activity of hexobarbital hydroxylase and hexobarbital-induced sleep time, in senescent male mice was similar to that in ...

journal_title：Biochemical pharmacology

authors： Niedermeyer TM,Shapiro BH

更新日期：1988-01-15 00:00:00

abstract：:The cytoprotective effect of the natural dietary constituent indole-3-carbinol (I-3-C) on carbon tetrachloride (CCl4) mediated hepatotoxicity in mice was examined. I-3-C pretreatment by gavage 1 hr prior to intraperitoneal injection of CCl4 produced a 63% decrease in CCl4-mediated centrolobular necrosis and a related ...

journal_title：Biochemical pharmacology

authors： Shertzer HG,Berger ML,Tabor MW

更新日期：1988-01-15 00:00:00

abstract：:Porcine cerebral microvessels were isolated by differential sieving and centrifugation and were characterized by microscopic examination and marker enzyme enrichment (gamma-glutamyltransferase; EC 2.3.2.2). Purified microvessels contained a membrane-bound enzyme immunologically indistinguishable from renal aminopeptid...

journal_title：Biochemical pharmacology

authors： Bausback HH,Churchill L,Ward PE

更新日期：1988-01-15 00:00:00

abstract：:Membrane damage caused by phospholipase A action is thought to be an important factor in ischemic myocardial injury. Propranolol has been shown previously to have beneficial effects in both animal experiments and clinical trials, and it has membrane-stabilizing properties in vitro. To investigate the possibility that ...

journal_title：Biochemical pharmacology

authors： Trotz M,Jellison EJ,Hostetler KY

更新日期：1987-12-15 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：:The genetically controlled polymorphic oxidation of debrisoquine and sparteine is caused by the absence or functional deficiency of a cytochrome P-450 isozyme. In order to elucidate the mechanisms underlying the differences in cytochrome P-450 function we have studied the 1'-hydroxylation of the prototype drug bufural...

journal_title：Biochemical pharmacology

authors： Dayer P,Kronbach T,Eichelbaum M,Meyer UA

更新日期：1987-12-01 00:00:00

abstract：:The binding of nimodipine, a 1,4-dihydropyridine Ca2+ channel antagonist, and of Bay K 8644, a Ca2+ channel activator, was measured in several regions of rat brain and compared to the distribution of K+ depolarization-induced 45Ca2+ uptake into synaptosomes. The maximum binding densities (Bmax) of [3H]nimodipine and [...

journal_title：Biochemical pharmacology

authors： Skattebøl A,Triggle DJ

更新日期：1987-12-01 00:00:00

abstract：:The carboxylesterase activity in both plasma and liver of guinea-pig were separated into three main peaks by chromatofocusing. Two of the three plasma enzymes were retained by affinity chromatography on Affi-Gel Blue (100-200 mesh). Isoelectric points determined by chromatofocusing or isoelectrofocusing were pI 6.1, p...

journal_title：Biochemical pharmacology

authors： Sterri SH,Fonnum F

更新日期：1987-11-15 00:00:00

abstract：:Dopamine can exist in both charged and uncharged forms at physiological pH. At present it is unclear which of these forms is responsible for dopaminergic agonist activity. The purpose of this study was to determine whether permanently charged structural analogs of dopamine containing either a nitrogen, sulfur, or sele...

journal_title：Biochemical pharmacology

authors： Wallace RA,Farooqui T,Wallace L,Ares J,Chang YA,Miller D,Uretsky N

更新日期：1987-11-15 00:00:00

abstract：:Diisopropyl-1,3-dithiol-2-ylidenemalonate (malotilate) was studied for and compared with cyanidanol, hydrocortisone and colchicin on its impact on fibroblast cultures. Under in vitro conditions, malotilate specifically reduces collagen synthesis of fibroblasts. In addition, malotilate is an efficient inhibitor of fibr...

journal_title：Biochemical pharmacology

authors： Poeschl A,Rehn D,Dumont JM,Mueller PK,Hennings G

更新日期：1987-11-15 00:00:00

abstract：:Hepatic microsomal glucuronoconjugation of the hypolipidemic drug clofibric acid was characterized in human liver and compared to the acylglucuronide formation of an endogenous substrate, bilirubin. The affinity of UDP-glucuronosyltransferase for bilirubin was 15-fold higher than for clofibric acid; the Vmax for the t...

journal_title：Biochemical pharmacology

authors： Dragacci S,Hamar-Hansen C,Fournel-Gigleux S,Lafaurie C,Magdalou J,Siest G

更新日期：1987-11-15 00:00:00

abstract：:In order to understand the relationship between the free ionized calcium concentration in the axon terminals and the transmitter release we have investigated the effect of ruthenium red (RuR) and m-chloro-carbonylcyanide phenyl hydrazon (CCCP), mitochondrial uncoupler agents on the liberation of acetylcholine from mye...

journal_title：Biochemical pharmacology

authors： Bernath S,Vizi ES

更新日期：1987-11-01 00:00:00

abstract：:Within the tissue surrounding the necrotic lesion, following a cryogenic injury of the brain, there is a definite activation of phospholipase A2 (at 2 and 4 hr post lesion) that accounts, at least in part, for the phospholipid breakdown. There is also an activation of cholinephosphotransferase (at 2 hr post lesion) th...

journal_title：Biochemical pharmacology

authors： Arrigoni E,Averet N,Cohadon F

更新日期：1987-11-01 00:00:00

abstract：:Milrinone [2-methyl-5-cyano-(3,4'-bipyridin)-6(1H)-one] is a positive cardiac inotropic agent recently shown to have thyromimetic activity in vitro in a rabbit myocardial membrane Ca2+-ATPase system [K. M. Mylotte et al., Proc. natn. Acad. Sci. U.S.A. 82, 7974 (1985)]. In the present studies, milrinone was examined fo...

journal_title：Biochemical pharmacology

authors： Davis PJ,Cody V,Davis FB,Warnick PR,Schoenl M,Edwards L

更新日期：1987-11-01 00:00:00

abstract：:An inhibitor of diacylglycerol kinase, R59022, enhanced activation of the neutrophil oxidase stimulated by the Ca2+-ionophore, A23187 (1 microM), and by N-formyl-methionyl leucyl-phenylalanine (1 microM). The enhancement was reversed by two inhibitors of c-kinase, retinal (10 microM), and gossypol (20 microM). Activat...

journal_title：Biochemical pharmacology

authors： Cooke E,Al-Mohanna FA,Hallett MB

更新日期：1987-10-15 00:00:00

abstract：:The effects of beta 1- and beta 1 + beta 2-antagonists on the myocardial adaptation to exercise training were investigated in male Sprague-Dawley rats randomly divided into trained (treadmill, 1 hr/day, 5 days/week for 10 weeks at 27 m/min, 15% grade) without drug (TC), sedentary without drug (SC), trained treated wit...

journal_title：Biochemical pharmacology

authors： Ji LL,Stratman FW,Lardy HA

更新日期：1987-10-15 00:00:00

abstract：:The disposition and metabolic fate of benzylpenicillin conjugated to a protein, human serum albumin (HSA), were compared with those of free penicillin in the rat. The conjugate was prepared by in vitro incubation of [3H]-benzylpenicillin and HSA at pH 10.8 for 24 hr at 37 degrees, conditions which favour the formation...

journal_title：Biochemical pharmacology

authors： Christie G,Kitteringham NR,Park BK

更新日期：1987-10-15 00:00:00

abstract：:Under certain modulating conditions the liver of the male Syrian golden hamster is a target organ for the carcinogenic effect of the synthetic estrogen diethylstilbestrol (DES). As a basis for mechanistic studies aimed at elucidating the role of metabolic activation in the process of DES-induced neoplasia, the metabol...

journal_title：Biochemical pharmacology

authors： Blaich G,Pfaff E,Metzler M

更新日期：1987-10-01 00:00:00

abstract：:The effects of antiulcer drugs, sofalcone and sucralfate, on the activity of gastric mucosal mucus glycoprotein fatty acyltransferase were investigated. The acyltransferase enzyme, contained in the detergent extracts of the microsomal fraction of rat gastric mucosa, was incubated with the deacylated gastric mucin and ...

journal_title：Biochemical pharmacology

authors： Slomiany BL,Liau YH,Mizuta K,Slomiany A

更新日期：1987-10-01 00:00:00

abstract：:The relationship between cytotoxicity and fluoropyrimidine effects on the production of mature cytoplasmic 28S and 18S ribosomal RNA was studied in S-180 cells for the fluoropyrimidines: 5-fluorouracil (FUra), 5-fluorouridine (FUrd), 5-fluorodeoxyuridine (FdUrd), and 5'-deoxy-5-fluorouridine (5'-dFUrd). After a 6-hr d...

journal_title：Biochemical pharmacology

authors： Takimoto CH,Tan YY,Cadman EC,Armstrong RD

更新日期：1987-10-01 00:00:00

abstract：:The calcium-ionophore A23187 causes a reversible increase of the hydrostatic pressure in the portal vein of perfused rat liver. Concomitantly, hepatic functions like the production of bile and the transhepatic movement of the bile acid taurocholate are diminished, mainly due to decreased uptake. These phenomena are pa...

journal_title：Biochemical pharmacology

authors： Akerboom T,Lenzen R,Schneider I,Sies H

更新日期：1987-09-15 00:00:00

abstract：:The characteristics of the muscarinic receptor in isolated gastric fundic cells from rabbit were determined by radioligand binding techniques and functional tests. The dissociation constants (KDS) of selective (hexahydrosiladifenidol and pirenzepine) and non-selective (N-methylscopolamine and atropine) muscarinic rece...

journal_title：Biochemical pharmacology

authors： Baudiere B,Monferini E,Giraldo E,Ladinsky H,Bali JP

更新日期：1987-09-15 00:00:00

abstract：:The role of calcium in the stimulation of phosphoinositide (PIn) hydrolysis by norepinephrine and the calcium ionophore A23187 was investigated in chopped cerebral cortex in which the PIns had been labeled previously with ([3H]myo-inositol. The accumulation of the newly formed [3H]inositol phosphate ([3H]IPs) was used...

journal_title：Biochemical pharmacology

authors： Knepper SM,Rutledge CO

更新日期：1987-09-15 00:00:00

abstract：:2-Fluoroadenine (F-Ade) is a metabolite of 9-beta-D-arabinofuranosyl-2-fluoroadenine (F-ara-A) that may be involved in the development of toxic side effects from this anticancer drug. The liberation of F-Ade from F-ara-A has been examined in different biological systems. Extracts of Escherichia coli but not mammalian ...

journal_title：Biochemical pharmacology

authors： Huang P,Plunkett W

更新日期：1987-09-15 00:00:00