Search results for "Adenylyl Cyclase Inhibitors"
showing 5 items of 5 documents
Purification and characterization of two exopolyphosphatases from the marine sponge Tethya lyncurium
1995
Abstract Two exopolyphosphatases (exopolyphosphatase I and II; EC 3.6.1.11) which release orthophosphate from inorganic polyphosphates have been detected and purified for the first time from a marine sponge, Tethya lyncurium . Exopolyphosphatase I has a molecular mass of 45 kDa, a pH optimum of 5.0 and does not require divalent cations for activity, while exopolyphosphatase II has a molecular mass of 70 kDa, a pH optimum of 7.5 and displays optimal activity in the presence of Mg 2+ ions. Final purification of the enzymes could be achieved by affinity chromatography on polyphosphate-modified zirconia. The mode of action of both enzymes was found to be processive. Orthophosphate is the sole p…
Mechanisms underlying the inhibitory effects induced by pituitary adenylate cyclase-activating peptide in mouse ileum
2005
Abstract The aim of this study was to investigate the signal transduction mechanisms underlying the inhibitory effect induced by pituitary adenylate cyclase activating peptide (PACAP-27) on the spontaneous contractile activity of longitudinal muscle of mouse ileum. Mechanical activity of ileal segments was recorded isometrically in vitro. PACAP-27 produced apamin-sensitive reduction of the amplitude of the spontaneous contractions. 9-(Tetrahydro-2-furanyl)-9H-purin-6-amine (SQ 22,536), adenylate cyclase inhibitor, or genistein and tyrphostin 25, tyrosine kinase inhibitors, had negligible effects on PACAP-27-induced inhibition. PACAP-27 effects were significantly inhibited by U-73122, phopho…
Synergistic platelet antiaggregatory effects of the adenylate cyclase activator iloprost and the guanylate cyclase activating agent SIN-1 in vivo
1993
The aim of our study was to evaluate the platelet antiaggregatory and hemodynamic effects of the stable prostacyclin analog iloprost and the NO-donor SIN-1, an active metabolite of molsidomine. The number of circulating platelets was determined in anesthetized male Wistar rats as a measure of in vivo platelet aggregation. Platelet count decreased from 648 +/- 25 to 476 +/- 15 x 10(3) platelets/microliter and from 578 +/- 36 to 411 +/- 40 (mean +/- SEM) in response to two repetitive injections of collagen (70 micrograms/kg body weight). Treatment with SIN-1 bolus injections (0.3 or 1 mg/kg bw) and/or continuous i.v. infusion of iloprost (0.2 or 0.4 micrograms/kg bw/min) was initiated 15 min …
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
1999
The distribution of tricyclic antidepressants from plasma to brain, where these drugs exert their main clinical action, and other organs is related to transport events across the cell membranes of the different tissues. It could be expected that all the molecular features that condition the transport processes (mainly hydrophobicity and molar total charge) also control the pharmacokinetic and biochemical behavior. Micellar liquid chromatography (MLC) has been proposed to emulate in vitro the partitioning process in the biomembranes. The use of micellar solutions of Brij35 as mobile phases in reversed-phase liquid chromatography has proven to be valid to predict the biological activities of …
Effects of sodium fluoride on the mechanical activity in mouse gastric preparations.
2005
The aim of the present study was to investigate the responses induced by sodium fluoride (NaF) on gastric mechanical activity, using mouse whole-stomach preparations. The mechanical activity was recorded in vitro as changes of intraluminal pressure. In most of the preparations, NaF induced a tetrodotoxin-insensitive biphasic effect characterized by early relaxation followed by slowly developing contractile response. The contraction was dependent on the concentration of NaF, whereas the relaxation was observed at only 10–30 mmol/L NaF. The contractile effect was significantly reduced by nifedipine (an L-type Ca2+channel blocker), ryanodine or ruthenium red (inhibitors of Ca2+release from sar…