Showing papers in "Biochemical Pharmacology in 1983"

TL;DR: The few existing reports on the careful pharmacodynamic, pharmacokinetic and clinical studies which have been made have been summarized to provide a basis for a full-scale investigation of the therapeutic potential of flavonoids.

TL;DR: The amount of glutathione present in hepatic protein mixed disulfides was determined to be 20-30 nmole/g liver and a newly developed test using GSH transferase and 1-chloro-2,4-dinitrobenzene for the estimation of GSH released from proteins after borohydride treatment was confirmed by HPLC analysis.

TL;DR: Inhibition of [3H]nitrendipine binding and blockade of K+ responses in guinea pig ileum by 1,4-dihydropyridines are well correlated, supporting the view that the observed binding is to Ca2+ channel.

TL;DR: Enhanced hepatocyte damage observed after treatment with a combination of ADR andBCNU versus BCNU or ADR alone is due to the extensive depletion of mitochondrial glutathione supported by ADR after glutathion reductase inhibition, which is strongly implicated in the mechanism of adriamycin toxicity.

TL;DR: These studies demonstrate that certain progestins in common clinical use probably possess inherent glucocorticoid activity and suggest that side effects attributable to this character might be expected when these compounds are used in pharmacological doses.

TL;DR: The PMN count in the sponges and the concentrations of both LTB4 and TXB2, but not PGE2, were significantly reduced by prior treatment of the animals with colchicine, which suggests that PMN are the major source of L TB4 andTXB2 in the inflammatory exudate whereas P GE2 is produced in significant amounts by other tissues.

TL;DR: The present findings with fluoxetine are consistent with the virtual absence of anticholinergic or other side effects often observed with tricyclic antidepressant drugs in animal models or during the treatment of depressed patients.

TL;DR: Results suggest that alterations in membrane integrity can be considered the cause underlying the well-known disturbances in renal function commonly observed during the initiation phase of HgCl2 and maleate induced acute renal failure.

TL;DR: Various 5-substituted-2'-deoxyuridines (dUrd) were shown to be effective substrates for the thymidine (dThd) phosphorylase isolated from human blood platelets and the highly potent and selective antiherpes agent (E)-5-(2-bromovinyl)-d Urd were degraded more rapidly than the natural substrates.

TL;DR: Human kidney TPMT activity could be distinguished from human kidney thiol methyltransferase (EC 2.1.9) activity on the basis of subcellular distribution, substrate specificity, kinetic characteristics and differential sensitivity to inhibitors.

TL;DR: The problems of esterase classification are discussed and some ideas presented to clarify the present confused state of the classification systems.

TL;DR: The alpha 2- and beta 2-character of the presynaptic receptors matches that of the corresponding extrajunctional receptors, which indicates that a circulating catecholamine, namely epinephrine, is involved in the regulation of adrenergic transmitter release.

TL;DR: Two flavonoids extracted from bilberries and a third one from grapes were demonstrated to protect collagen against this non-enzymatic proteolytic activity, confirming that collagen may be degraded during the process of inflammation and that some flavonoid are endowed with protective properties.

TL;DR: Results indicate that, in the presence of CB3717, thymidylate synthetase, rather than dihydrofolate reductase, became rate-limiting for the cycle of dihydofolate oxidation and reduction.

TL;DR: 2,6-pyridinediol and 6-benzyl-2-thiouracil have been identified as being potent inhibitors of UrdPase and dThdPase respectively.

TL;DR: The results of a study on the effects of several macrolide antibiotics including oleandomycin, erythromycin derivatives, josamycin, methymycin, tylosin, spiramycin and rifampicin as well as antibiotics of other series, such as tetracycline and lincomycin on rat liver cytochromes P-450 in vivo and in vitro are reported.

TL;DR: Challenge of rat peritoneal mast cells with anti-rat IgE induces a similar pattern of protein phosphorylation to that already reported for compound 48/80, and sodium cromoglycate appears to activate an endogenous control mechanism for switching off mediator release using a mechanism mediated by cGMP.

TL;DR: The results indicate that the recently identified phospholipid-sensitive species of Ca2+-dependent protein kinase was inhibited by a variety of agents, probably via their abilities to interfere with a hydrophobic interaction between phospholIPid and the enzyme, an interaction presumably required to confer upon the enzyme a Ca2+.

TL;DR: It is of more value to measure blood urea and ammonia concentrations routinely shortly after starting valproate therapy than to do conventional liver function tests, because it could significantly impair liver function when there is an additional insult.

TL;DR: It is concluded that the administration of erythromycin propionate induces microsomal enzymes and results in the formation of an inactive cytochrome P-450-metabolite complex in humans, however, the concn of uncomplexed (active) cyto chrome P- 450 and tests for in vitro and in vivo drug metabolism were not significantly modified.

TL;DR: It is useful to consider how the binding properties of drugs for other neurotransmitter receptors are affected by the intrinsic activity of the ligand, and the fundamental principle providing basis for these relationships is emphasized.

TL;DR: The structure-activity relationship observed for human lens enzyme was similar to that reported previously for rat lens enzyme, and inhibitory activity on the whole however, was lower with human lens enzymes.