Showing papers in "Biochemical Pharmacology in 1976"

TL;DR: Phospholipase is the key enzyme which mobilises free fatty acids for prostaglandin biosynthesis during these types of cell injury, indicating that substrate availability is not the only requirement for stimulation of prostaglanders biosynthesis.

TL;DR: The data of the present study are consistent with a role for the hydroxyl radical and appear to rule out a direct causative role for hydrogen peroxide, while other data rule out any protective role for transiently elevated levels of blood glucose resulting from the administered compounds.

TL;DR: In this paper, the authors present a brief review of the relationship between precursors and the rate at which a compound is synthesized in the brain and the amount of substrates required to reach full saturation.

TL;DR: It is suggested that the apparent selectivity exhibited by paraquat for the lung is associated with the accumulation process.

TL;DR: Flavonoids were found to be highly potent inhibitors of aldose reductase, the enzyme that initiates cataract formation in diabetes, and further search may reveal even more potent analogues of this ubiquitously distributed group of plant polyphenols.

TL;DR: The protein binding of diazepam, indomethacin, salicylic acid, sulfadimetoxine and warfarin in serum of uremic patients has been studied by equilibrium dialysis and circular dichroism measurements and compared with that in normal serum.

TL;DR: Mice tested 24 hr after EOS injection showed mild to moderate alaxia and were completely protected against ‘audiogenic’ seizures andBrain GABA concentration was increased 4–10 fold and GABA-transaminase activity was inhibited by 54–58% There was no inhibition of succinic Semialdehyde dehydrogenase activity.

TL;DR: The α-methyl-substituted amines dl-α-methylbenzylamine, d- α-methyltryptamine and the two stereoisomers of amphetamine were shown to be competitive inhibitors of the oxidation of benzylamines, tyramine and serotonin by rat liver monoamine oxidase.

TL;DR: Inhibition by amiodarone and propranolol of the chronotropic effect of isoproterenol on spontaneously beating rabbit right atria has been studied in vitro and phentolamine was shown to inhibit the adrenergic α receptor competitively.

TL;DR: Results indicate that blood acetaldehyde levels after acute administration of ethanol do not reflect those found in brain, and suggest that brain may be protected, at least in part, from concentrations of acetaldehyde found in blood, by an effective metabolic barrier.

TL;DR: The experiments demonstrate conclusively that CCl 3 -Cl bond cleavage and covalent binding of products of CCl 4 metabolism do not constitute a mechanism for loss of microsomal glucose 6-phosphatase, cytochrome P-450 or aminopyrine demethylase for the particular anaerobic conditions employed in vitro.

TL;DR: Bovine Superoxide dismutase administered intravenously to rats, completely suppressed the prostaglandin phase swelling of carrageenan foot-oedema, but had no effect on the histamine and serotonin phase.

TL;DR: Two epoxide-metabolizing enzymes, glutathione- S -epoxide transferase and epoxide hydrase, were studied in subcellular fractions of rabbit liver, lungs, intestinal mucosa and kidney and species did not differ markedly when the same organ was compared in rabbits, rats and guinea pigs.

TL;DR: It was found that for a substance to exhibit biologic activity it must contain the two aromatic ring systems and the phenyl ring must hear methoxy groups.

TL;DR: Cyanamide (H 2 N—C  N) is effective as an agent to treat alcoholism presumably because it inhibits aldehyde dehydrogenase, but less effective against the brain enzymes.

TL;DR: Equations have been developed which provide the basis for the elucidation of the inhibition mechanism of a tight-binding inhibitor by studying the manner in which the substrate interferes with the bincling of the inhibitor to the enzyme, and it is demonstrated that coformycin competes with adenosine forAdenosine deaminase from calf intestinal mucosa.

TL;DR: The biological activity of the sulphate ester of 3-hydroxybenzo(a)pyrene is of interest as this metabolite could be extremely persistent in man because of its physico-chemical properties, which may prevent its excretion in the urine and bile.

TL;DR: The results indicate that the dopamine nerve terminals of the corpus striatum possess greater stereoselectivity toward amphetamine than either the norepinephrine nerve terminal of cerebral cortex or 5-hydroxytryptaminc neurons of midbrain.

TL;DR: NMR binding measurements have been performed in order to analyze the molecular mechanism underlying the drug-induced phospholipidosis, and increasing lipophilicity is correlated with an increase in binding for this type of amphiphilic drugs.

TL;DR: Evidence has been obtained that only aryltriazenes that can be metabolized in vivo to an aryl- N 3 -monomethyltRIazene have anti-tumour properties.

TL;DR: Drug-induced receptor binding enhancement appears to involve an increase in number of binding sites rather than a change in receptor affinity, and naloxone is the most potent drug in producing receptor enhancement.

TL;DR: Kallikrein activity in 81 human urine samples and 8 samples obtained from a dog undergoing stop-flow procedure was measured by RIA and bioassay and the RIA was sensitive to 10 pg kinins, and the two displacement curves for [ 125 I]bradykinin were similar.