Showing papers in "Biochemical Pharmacology in 1970"

TL;DR: The time-course of effects of a single dose of p -chlorophenylanine on rat brain amines shows a significant lowering of serotonin (5HT) and 5-hydroxyindole-3-acetic acid (5HIAA) beginning on day 1 and lasting for about 8 days.

TL;DR: It was suggested that if the persistent inhibitory action on DNA synthesis is directly related to the chemotherapeutic efficacy of this agent or a metabolic product thereof, a less frequent treatment regimen may be as effective as daily injections while evoking fewer toxic reactions.

TL;DR: Qualitative and quantitative investigations on the metabolism in rat-liver preparations of eleven tritiated hydrocarbons showed that all the major ethyl acetate-soluble metabolites of these Hydrocarbons have been recognised: in most cases the structure of the metabolites have been confirmed.

TL;DR: Physostigmine plus atropine gave rather more protection to guinea pigs against Sarin but not so much as was given by P2S (2-hydroxyiminomethyl-N-methylpyridinium methanesulphonate) and atropines.

TL;DR: It has been shown that 1-[14C]acrylamide reacts in vivo and in vitro with non-protein sulphydryl and with proteins of rat tissue, and in contrast to this similar reactivity, N-(hydroxymethyl) acrylamides does not produce peripheral neuropathy.

TL;DR: Gas chromatographic analysis of bovine, cat, rat and guinea pig brain extracts revealed the presence of a compound with properties identical to those of γ-hydroxybutyrate.

TL;DR: Since dopamineβ-hydroxylase activity in adrenal medulla was found to be inhibited in vivo after the administration of fusaric acid, the decrease in the catecholamine levels is attributed to the inhibition of norepinephrine synthesis at the dopamine β-Hydroxylases stage.

TL;DR: Nonsteroidal anti-inflammatory agents inhibited the heat denaturation of serum albumin at drug levels betow 1 mM, as measured by turbidity and viscosity changes.

TL;DR: The results suggest that the reduction of 4-NQO to 4-HAQO is carried out mainly by DT diaphorase, but p-NBA is reduced by usual nitro reductase, which seems to be a responsible factor for 4- NQO carcinogenesis.

TL;DR: The release of inorganic mercury was found to be the major biotransformation pathway available for methylmercury salts in rats and this role is discussed with reference to the biochemical mode of action and the pharmacokinetics of these very hazardous compounds.

TL;DR: Observations are suggestive that GBL increases brain dopamine primarily by selectively blocking the release of this monoamine from dopamine containing neurons by way of a blockade in dopamine release induced by GHB.

TL;DR: The inhibitor SKF-525A differentiated between the demethylase activities present in the two types of induced animals, inhibited the activity found in microsomes of phenobarbital-induced rats but had little effect on the activity inmicrosomes from 3-methylcholanthrene-treated rats.

TL;DR: The half-life of radioactivity in blood after an intravenous injection of Δ1-tetrahydrocannabinol-3H ranged from 7 to 16 min this paper, and 30 min after i.v. administration of †1-triggered 3H, only 3-4 per cent of the radioactivity was due to unchanged compound.

TL;DR: The evidence favors the hypothesis that at least two forms of GAD exist in animal tissues, and Pyruvate was the most effective organic anion tested in stimulating the kidney enzyme and was more effective than isomolar concentrations of Cl−.

TL;DR: Tritiated K-region epoxides of phenanthrene and dibenz[a,h]anthracene reacted with DNA, RNA and histone on incubation at 37° but the parent hydrocarbons and their respective K- Region dihydrodiols did not react.

TL;DR: The binding of tritium-labelled Δ1-tetrahydrocannabinol to human plasma proteins in vitro was studied with electrophoretic techniques and was found to be associated to 80–95 per cent with lipoproteins.

TL;DR: Both categories of drug influence 5-HT metabolism, and the noted differences with respect to 5-HIAA cannot as yet be accounted for.

TL;DR: It was found that the release of two bromide ions from EDB required stoichiometric amounts of GSH, and S-(β-hydroxyethyl) glutathione has been identified as the major product formed in vitro.

TL;DR: The results suggest that androgens increase the affinity of P-450 for the binding with substrates and estrogens directly counteract the action of androgen, consequently the alteration of the activities of drug oxidations may occur.

TL;DR: Investigation of sucrose homogenates of guinea pig brain demonstrated that very little GHB was found associated with the particulate fraction and administration of ethanol caused a marked increase in tissue levels of GHB, presumably by facilitating the reduction of succinic semialdehyde.

TL;DR: Microsomes from houseflies and from the livers of rats, pigs and rabbits hydrate enzymically the epoxide rings of several cyclodiene type insecticides, resulting in the hydration of mainly one enantiomeric form and permitting partial resolution of the racemates.

TL;DR: None of the metabolites examined significantly affected the in vitro activity of either of the 5HT synthesising enzymes tryptophan 5-hydroxylase and 5-Hydroxytryptophan decarboxylase.

TL;DR: The action of MDP synergists and related compounds in increasing drug and insecticide potency possibly is the result of combination of the MDP compound with an active site on the mixed-function oxidases resulting in inhibition of normal detoxification mechanisms.

TL;DR: It has been shown that oxyphenbutazone has an extra binding site possibly involving a hydrogen bond to imidazolium ion in the protein, and association constants for these systems have been determined.

TL;DR: During a period of 15 days following induction of adjuvant arthritis in rats, the liver microsomal N -demethylase and NADPH 2 -oxidase enzyme activity and levels of cytochrome P-450 are greatly reduced, implying a reduced capacity for the oxidative metabolism of steroids and foreign compounds in adjuant arthritic rats which should influence the toxicity and half-life of any administered compound.

TL;DR: 7,12-Dimethylbenz[a]anthracene was converted by mouse embryo cells into its 8,9-dihydrodiol and into the 7-hydroxymethyl derivatives of the corresponding hydroxymethy derivatives, probably by a non-enzymic reaction.

TL;DR: The effects of EDS may indicate that both compounds have latent “mustard-like” activity, and this possibility is discussed in terms of the pharmacological effects produced by EDS and its chemical reactions with nucleophiles.

TL;DR: It was shown that neuroactive drugs added to the perfusion fluid promoted the release of labeled vitamin and that whereas in the nerve preparations the bulk of the vitamin was in the form of the di- or triphosphate, the released material consisted of free thiamine andThiamine monophosphate.