... receptors. We previously identified a selective small molecule ligand, compound 2, that acted as a full agonist and allosteric modulator of GLP-1R. In this study, the structurally related small molecule, compound 3, stimulated cAMP production from GLP-1R, but not from the homologous glucagon receptor (GluR...

... in a dose-dependent manner. Papaverine increased the cyclic adenosine monophosphate (cAMP) but not cyclic guanosine monophosphate (cGMP) content. IBMX, Db-cAMP and 8-br-cGMP did not affect twitches, whereas verapamil and NaCN inhibited twitches. Increases in extracellular Ca 2+ removed the twitch inhibition...

...Mathew S. Eapen; Reena Sodhi; Gayathri Balakrishnan; Sunanda Dastidar; Abhijit Ray; Lalitha Vijayakrishnan Phosphodiesterases (PDE) are enzymes that catalyze the hydrolysis of cAMP/cGMP to 5′-AMP/GMP. In vitro assays have routinely assayed cAMP/cGMP levels as a direct indicator of PDE activity...

... Cardiomyocytes R-metoprolol S-metoprolol RS-metoprolol ERK cAMP Abstract Background/Aims: Since -adrenoceptors have been shown to affect cardiac gap junction channels, we wanted to elucidate the possible effect of metoprolol on the gap junction protein connexin-43, using racemic RS-metoprolol...

... rats. Sham-operated rats served as controls. Hemodynamic and cyclic nucleotide measurements were performed at 14 days after surgery. The portal venous pressure was significantly higher, while systemic arterial pressure and heart rate were lower in PVL rats than those in controls. Basal cAMP (PVL, 10.91...

...Manuel Sánchez; Luis Menéndez; Maria José García de Boto; Agustín Hidalgo The effects of phosphodiesterase inhibitors, an activator and an inhibitor of guanylyl cyclase, and cAMP and cGMP analogs on oxytocin-induced contractions have been studied in the testicular capsule of rats. The nonspecific...

... the oxymetazoline-induced ocular hypotensive response. Oxymetazoline induced mydriasis in treated eyes at all doses. In in vitro studies, oxymetazoline inhibited isoproterenol-stimulated cAMP production in rabbit iris-ciliary bodies and cultured rabbit nonpigmented ciliary epithelial cells. The inhibition of cAMP...

...Richard M. Edwards; Elwood J. Stack; Miklos Gellai; David P. Brooks The ability of α 2 adrenoceptor agonists to inhibit vasopressin (VP)-stimulated cAMP accumulation in collecting tubules and to inhibit the antidiuretic effect of VP in rats is clearly established. However, in other species...

... increases in cAMP formation in membrane particles from superior mesenteric artery and its main branches. The presence of both SCH 23390 and propranolol was required to completely abolish dopexamine-induced increases in cAMP formation. In functional studies, dopexamine (1 and 3 μg/kg/min) produced dose...

...Neil P. Lewis; Douglas R. Ferguson 3 H-Angiotensin II binding was studied in rat renal proximal tubular basolateral membranes. The characteristics of binding were found to be consistent with a receptor for angiotensin II at this site. Effects of angiotensin II on cAMP production were studied...

...U. Havemann; K. Kuschinsky In slices of rat striata, incubated in a depolarizing medium (53 mM K + ), morphine decreased the concentration of cAMP even in concentrations as low as 0.5 μM . This effect was inhibited by naloxone. Levorphanol, but not dextrorphan, induced a similar effect as morphine...

... (5, 10 and 20 mg/kg intravenously) on HCl secretion and cAMP content of gastric juice in pyloric and cardiac ligated male Sprague-Dawley rats was investigated. Compared with the control group, halothane significantly increased both HCl secretion and cAMP content of gastric juice, but to a lesser...

... and Neurological Disorders1 K. Fuxe, B.B. Fredholm, L.F. Agnati, S.-O. Ogren, B.J. Everitt, G. Jonsson and J.-A. Gustafsson Departments of Histology, Pharmacology and Chemistry, Karolinska Institutet, Stockholm, and Astra Pharmaceuticals AB, Sôdertalje Key Words. Behaviour cAMP Ergot drugs Monoamines...

... advertised or of their effectiveness, quality or safety. The publisher and the editor(s) disclaim responsibility for any injury to persons or property resulting from any ideas, methods, instructions or products referred to in the content or advertisements. Adenylate cyclase Bromocriptine cAMP...

...H. Osswald; A. Hawlina Changes in tissue levels of cyclic adenosine 3’:5’-monophosphate (cAMP) and cyclic guanosine 3’:5’-monophosphate (cGMP) in the rat kidney in response to acid-base changes and administration of acetazolamide were measured. cAMP was determined according to the method described...

...E. Arrigoni-Martelli; E. Bramm; L. Binderup The injection of 50 μg i.p. of actinomycin D produces, in rats, a biphasic inflammatory reaction. The first short lasting phase (∼24 h) is characterized by the decrease of the peritoneal cells number, by the increase of the levels of both cAMP and cGMP...

... in the signal transduction system are complex. While DPT alone (0.1–1,000 µmol/l) activates G i when both cAMP and γ-S-GTP incorporation are measured, in the presence of 5-HT (0.1–10 µmol/l), DPT blocks the agonist effect. In combination, the findings suggest that DPT is a moderate affinity partial agonist...

...-( o -methoxyphenyl)piperazin-1-yl]-methyl]-1.3-dioxoperhydroimidazo[1.5-a]pyridine (B-20991), an arylpiperazine derivative, have now been further studied. B-20991 was found to antagonize the forskolin-induced increase of cAMP synthesis in a HeLa cell line transfected with the human 5-HT 1A...

...-dependently inhibited histamine release in the peritoneal mast cells activated by compound 48/80 or anti-DNP IgE. All of these effects were comparable to those of the disodium cromoglycate (reference drug) tested. When sulfasalazine was added, the level of cAMP in rat peritoneal mast cells transiently...