Showing papers in "Biochemical Pharmacology in 1986"

TL;DR: The novel bicyclic compound Wy-45,030 exhibited a neurochemical profile predictive of antidepressant activity that was not antimuscarinic in the guinea pig ileum, nor did it have any appreciable affinity for brain alpha-1 adrenergic or histamine-1 binding sites.

TL;DR: The results show that the three forms of PDE isolated from aortic smooth muscle retain properties that they exhibit in the tissue and which are similar in the three species examined, including man, suggesting that each form participates in a specific manner to the regulation of cAMP and cGMP concentrations in aorta smooth muscle cells.

TL;DR: Preliminary data indicated a significant correlation between the potencies of cocaine congeners in inhibiting the Na+-dependent binding of [3H]cocaine and their potencies in inducing stereotyped sniffing upon intraventricular administration.

TL;DR: Heterogeneity regarding the number of phosphodiesterases present in various tissue/cell types, as well as their substrate specificity and their ability to be stimulated by calmodulin are demonstrated, and these different molecular forms ofosphodiesterase can be selectively inhibited by different pharmacological agents.

TL;DR: The present investigation suggests that zinc may induce the increase in alkaline phosphatase related to DNA synthesis and, as a result, stimulate bone growth.

TL;DR: Evidence is presented that the mitochondrial respiratory bursts induced by both flavonols and their auto-oxidation resulted in the generation of O-2 and H2O2.

TL;DR: agents that inhibit gamma-glutamyl transpeptidase, cysteine conjugate beta-lyase, and renal organic anion transport systems, namely L-(alpha S,5S)-alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid, and probenecid protected against S-conjugate-induced nephrotoxicity.

TL;DR: The data indicate that the density of distribution of beta-adrenergic receptors was not homogeneous on the precursors of phenotypically and functionally distinct T cells, suggesting that the receptors were mainly of the beta-2 type.

TL;DR: In this article, the authors showed that the desensitization of guanylate cyclase to activation by nitrovasodilators represents a stable alteration of the enzyme.

TL;DR: Alveolar type II cells can supplement endogenous synthesis of GSH with uptake of exogenous GSH to protect against paraquat-induced injury, and addition of inhibitors of this transport system prevented the protection against injury afforded by GSH.

TL;DR: This work directly compared the abilities of three bipyridyl herbicides, diquat (DQ), paraquat (PQ) and benzyl viologen (BV), to generate superoxide anion radical (O2-.) in rat liver microsomes and H2O2 in hepatocytes and correlated this with their relative toxicities to a compromised isolated hepatocyte system.

TL;DR: It is demonstrated that ketoconazole is a comparatively specific and orally active inhibitor of the 5-lipoxygenase activity bearing on the production of leukotrienes derived from arachidonic acid.

TL;DR: The rapid rate and extensive accumulation of chloroquine, and the lack of significant alkalinization, indicate that a new theory of the mechanism of antimalarial action of the drug is required.

TL;DR: The broad specificity of carbonyl reduct enzyme for quinones is in keeping with a role of the enzyme as a general quinone reductase in the catabolism of these compounds.

TL;DR: Results are consistent with tamoxifen inhibition of PKC function in intact human cells as assessment of cell integrity by the exclusion of trypan blue and measurement of intracellular concentrations of ATP showed no significant differences.

TL;DR: In this article, the effects of administration of highly purified eicosapentaenoic acid (EPA) ethyl ester (79% pure) in two models of acute inflammation were assessed.

TL;DR: 2,3-diMe-1,4-NQ is not cytotoxic (except in the presence of dicoumarol) and this lack of toxicity may be related either to its lesser capacity to redox cycle and/or its inability to react directly with cellular nucleophiles.

TL;DR: The molecular geometries of specific substrates, inhibitors and inducers of cytochrome P-448 activity were determined using computer-graphic techniques for use in defining the molecular dimensions of the substrate binding site of this enzyme.

TL;DR: It is suggested that parasite feeding on host cell cytosol is the primary target for the antimalarial action of these drugs, and the metabolically dependent acidification of this parasite organelle is involved in both processes.

TL;DR: A kinetic plot of initial velocity versus [PLA2] supported the hypothesis that MLD apparently inactivates bee venom PLA2 by an irreversible mechanism.