Showing papers in "Biochemical Pharmacology in 1987"

TL;DR: Flavonols are anti-thrombotic because they are selectively bound to mural platelet thrombi and owing to their free radical scavenging properties resuscitate biosynthesis and action of endothelial prostacyclin and EDRF.

TL;DR: The findings indicate that the zinc had a direct stimulatory effect on bone mineralization in vitro, and that bone protein synthesis was a necessary component of this response.

TL;DR: Comparisons of the stereoisomers of methylenedioxymethamphetamine and its n-desmethyl analog, methylenedioxyamphetamine, indicated two phases of serotonin depletion similar to those reported for p-chloroamphetamine, and the (+)-enantiomer of both drugs to be the more potent releasing agent.

TL;DR: The results suggest that the formation of glutathione-protein mixed disulfides occurs as a result of increased GSSG formation and inhibition of glutATHione reductase activity during menadione metabolism in hepatocytes.

TL;DR: This review has highlighted some of the well-described differences in endothelial cells derived from different sites of the vascular tree, and the importance of the epithelium and/or epithelial basal lamina in the maintenance of endothelial ultrastructure was demonstrated in a developmental study of rat intestinal capillaries.

TL;DR: The reactions of several platinum antitumor agents with sulfur-containing amino acids, peptides, proteins, and nonbiologic nucleophiles are characterized and DDTC and thiourea were shown to restore activity to platinum-inhibited enzymes.

TL;DR: The in vitro and in vivo effects of these flavonoids and polyphenols may be related to their antioxidant abilities, making them promising substances to be investigated as water-soluble protectors against lipid peroxidation and other free radical-mediated cell injury.

TL;DR: Observations suggest that the N-1 substituent of an azole antifungal agent regulates the mobility of the molecule in the heme crevice of ferrous P-45014DM and determines the inhibitory effect of the compound.

TL;DR: Several alkyl phosphorylcholines and related derivatives were tested against Leishmania donovani amastigotes in mouse peritoneal macrophages in vitro and ED50 values were determined in the range of 1-12 microM.

TL;DR: Treatment with the GSH synthesis inhibitor BSO may preferentially enhance the cytotoxic effects of alkylating agents against human ovarian cancer and overcome acquired resistance.

TL;DR: The results suggest that MDMA and its homologs may be more closely related to amphetamine rather than to DOM in their biochemical mode of action.

TL;DR: Ketanserine and methiothepin, 5-HT receptor antagonists, did partially block the methylenedioxymethamphetamine-induced loss of tryptophan hydroxylase activity, suggesting a possible role for neurotransmitter release in the acute effects of the drug on enzyme activity.

TL;DR: 5-Aminosalicylate can protect alpha 1-antiprotease against attack by the myeloperoxidase-derived oxidant hypochlorous acid and may contribute to the anti-inflammatory action of sulphasalazine and its metabolites.

TL;DR: In the presence of a reporter substrate, the progressive inactivation of an enzyme was easily studied by directly transmitting absorbance readings to a microcomputer and the method was extended to the study of hysteresis phenomena.

TL;DR: Verapamil alone was much more toxic to multidrug resistant cells than to the sensitive cells, suggesting that calcium channel blockers are specifically toxic to MDR cells by virtue of an interaction with the MDR cell surface distinct from that involved in promoting cellular accumulation.

TL;DR: The impact of glucocorticoids on the brain is examined, placing particular emphasis on the interactions between glucoc Corticoids and biogenic amines, such as serotonin, dopamine and epinephrine, and their effects on mood and on behavior.

TL;DR: The results indicate that the major pharmacokinetic differences between Carboplatin and cisplatin relate to their renal handling and their reactivity with macromolecules.

TL;DR: It is found that homogenates of human liver contain at least two forms of PST that are similar to brain and platelet TL and TS PST with regard to substrate specificities, thermal stabilities and sensitivities to inhibitors, and that human liver contains two isozymes of TS PST.

TL;DR: It is suggested that sodium cholate and proteinase inhibitors can facilitate the absorption of intact, biologically active proteins across the intestinal wall.

TL;DR: Enhanced hepatic levels of glutathione protected in vivo against the damaging effects of AA, and the ferric iron chelator desferoxaminemethanesulfonate prevented AA-induced lipid peroxidation and liver cell damage in vivo.

TL;DR: Data indicate that, by using an antagonist radioligand to label 5-HT2 receptors and agonist radiolIGands to label 4-bromo-2,5-dimethoxyphenylisopropylamine, the5-HT1 receptor selectivity may be overestimated, which may be an especially severe problem in serotonin drug development as drugs that interact potently with 5- HT2 receptors have been reported to be psychoactive and/or hallucinogenic

TL;DR: The results suggest that the chloroethyl and methylimidazole-triazinones are similar to the nitrosoureas and triazenes in that cytotoxicity correlates with alkylation of the O6-position of guanine, while the ethyl analogues appear to produce an alternate cytotoxic lesion.