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Inhibitors of GlyT1 Affect Glycine Transport via Discrete Binding Sites
In GlyT1-expressing membranes, the binding of the novel radioligand [3H]N-methyl-SSR504734 to a single site on GlyT 1 was competitively displaced by glycine and SSR50 4734 but noncompetitively by sarcosine-based compounds, which indicates a noncompetitive mode of action.
The Vasopressin 1b Receptor Antagonist A-988315 Blocks Stress Effects on the Retrieval of Object-Recognition Memory
Findings indicate that direct antagonism of V1b receptors is an effective treatment to block stress-induced activation of the HPA axis and the consequent impairment of retrieval of different aspects of recognition memory.
Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs.
Successful attenuation of venous thrombus growth in rabbits after the administration of a novel oral thrombin inhibitor.
Intravenous administration of BSF 208791 showed superior antithrombotic properties as compared with Polyethylenglycol-Hirudin and low molecular weight heparin in a model of venous thrombosis in rabbits and bleeding time was less affected after administration.
Synthesis of a homologous series of ketomethylene arginyl pseudodipeptides and application to low molecular weight hirudin-like thrombin inhibitors.
The design of low molecular weight thrombin inhibitors IIa-d (hirutonins) that bind concurrently with the enzyme's catalytic site and auxiliary "anion-binding exosite" for fibrinogen recognition is reported and the bimolecular interactions served to explain the retention of high enzyme affinity.
Primary stimuli of icosanoid release inhibit arachidonoyl-CoA synthetase and lysophospholipid acyltransferase. Mechanism of action of hydrogen peroxide and methyl mercury in platelets.
It is concluded that the inhibitory effect of H2O2 and methyl mercury on the arachidonate-reacylating enzymes Arachidonoyl-CoA synthetase or lysophospholipid acyltransferase are responsible for their capacity to stimulate icosanoid release in intact cells.
Hydrogen Peroxide and Methyl Mercury are Primary Stimuli of Eicosanoid Release in Human Platelets
Hydrogen peroxide (H2O2) and methyl mercury induced the liberation of arachidonate and its metabolites from human washed platelets and suppressed the formation of [14C]eicosanoids, indicating that the platelet activation by H2O1 and methyl Mercury essentially requires previous PGH2/TXA2 formation.