Showing papers in "Biochemical Pharmacology in 1977"

TL;DR: Three ADA (adenosine deaminase) inhibitors, DHMPR, EHNA and deoxycoformycin (a transition state analog), were classified as readily reversible, semi-tight-binding and tight-binding inhibitors.

TL;DR: It is suggested that platelet MAO consists of essentially one distinguishable form of MAO which most closely resembles the MAO type B found in other tissues.

TL;DR: Phencyclidine was fairly similar in potency to d- methamphetamine and methylphenidate in inhibiting catecholamine uptake but was 8 times more potent than d-amphetamine and 34 times more powerful than methylphenidates in inhibite [3H]serotonin uptake.

TL;DR: The experiments indicate that rapid inactivation of enkephalins may be due to at least two different enzymes present in tissues.

TL;DR: The results of this study suggest that toluene exerted its protective effect by inhibiting benzene metabolism and that a metabolite of Benzene probably mediates the observed hemopietic toxicity of benzene.

TL;DR: 6-Methoxy-1,2,3,4-tetrahydro-β-carboline produced greater MAO inhibition with serotonin as the substrate than with β-phenylethylamine both in vitro and in vivo, suggesting that it is a relatively selective inhibitor of MAO type A.

TL;DR: The results indicate that the net uptake of anthracycline derivatives in these tumour cells is determined by the permeability of the membrane to the unionized form of the molecule, the specificity of the drug for the mechanism of active efflux, and the relationship between intracellular and extracellular pH.

TL;DR: The results showed that the liver was the primary site for the oxidation of the ethanol-derived AeH, and only a small amount of the total AcH formed in this organ escaped into the rest of the body, but this amount increased with increased hepatic ethanol concentration.

TL;DR: Using the recently developed sensitive assay with [3H] benzo [a] pyrene 4,5-oxide as substrate, epoxide hydratase was shown to be present in 26 rat organs and tissues investigated, supporting the assumption that in these organs a single enzyme is responsible for the hydration of both substrates—as was earlier shown by several methods for the rat liver.

TL;DR: The availability of tyrosine to the brain may be one of the factors normally controlling brain catecholamine synthesis, and neutral amino acids, valine and isoleucine, had no effect on tyrosin hydroxylase activity in vitro in concentrations up to 10−3 M.

TL;DR: The results suggest that sulfide produces death in animals by inhibition of cytochrome oxidase, but such a mechanism seems unlikely in the case of azide.

TL;DR: High concentrations of deoxycoformycin and EHNA inhibit all pathways of purine ribonucleotide synthesis, and inhibit the conversion of inosinate to adenine and guanine nucleotides.

TL;DR: Thymidine concentrations were determined in the serum and urine of different animal species and man with a sensitive microbiological method, using Lactobacillus arabinosus ATCC 8014 and in mice thymidine concentration was seen to be enhanced by infections.

TL;DR: It was demonstrated that the sulphydryl compounds β-mercaptoethylamine-HCl, cysteine and methionine significantly increased the survival rate of mice given a lethal dose of ethanol.

TL;DR: Silymarin, a 3-oxyflavone present in Silybum Marianum, protected both liver mitochondria and microsomes from lipid peroxide formation induced by various agents.

TL;DR: It is suggested that parenterally administered cadmium-thionein is taken up by the renal tubules and catabolized, probably by the lysosomes of the tubular cells, with the liberation of Cd 2 + ions.

TL;DR: It appears that both binding and inhibition depend on the accessibility of the non-bonded electrons on the nitrogen atom at position — 3 of the ring.

TL;DR: It was found that N -hydroxy-phenacetin became rapidly covalently bound after sulfation of the N -Hydroxy group, and of the covalent binding of its conjugates, were determined.

TL;DR: It is concluded that DF, BEX, DDTC and CS2 inhibit the N-oxidation in vivo of azomethane to azoxymethane, an essential step in the metabolic activation of 1,2-dimethylhydrazine.

TL;DR: Carnitine acetyl- and octanoyltransferases are the first reported enzymes whose peroxisomal specific activity increases with clofibrate treatment.

TL;DR: It is concluded that binding of the reactive metabolite of paracetamol to hepatocyte macromolecules need not lead to hepatic necrosis provided that sulphydryl groups are present in the liver to prevent the deleterious effects of such binding.

TL;DR: It is concluded that technical pentachlorophenol produces a number of liver changes which cannot be attributed to pentach chlorophenol itself, but are consistent with the effects of biologically active chlorinated dibenzo-p-dioxins and dibenzofurans.

TL;DR: Both the incorporation rates of precursors of DNA- and RNA synthesis, as well as of protein synthesis are in intact cells inhibited by Virazole, and already 2 hr after incubation with the drug the amount of polyribosomes decreases.