Because of the complexity derived from the existence of various phosphoinositide 3-kinase (PI3K) isoforms and their differential roles in cancers, development of PI3K inhibitors with differential pharmacologic and pharmacokinetic profiles would allow best exploration in different indications, combinations, and dosing regimens. Here, we report BAY 80-6946, a highly selective and potent pan-class...

We carried out a study of the spatial and temporal effects of land-derived material on water column nutrients and plankton dynamics in a subtropical estuary. The study had 2 parts: (1) a 3 yr synoptic monitoring program, and (2) a shorter 1.5 yr study during the second half of the program, which focused on individual pulses driven by discrete rainfall events. Although we found spatial differenc...

BAY y 5959 is a dihydropyridine derivative that binds to L-type calcium channels in a voltage-dependent manner and promotes calcium entry into the cell during the plateau of the action potential by influencing mean open time. Because myofilament responsiveness to calcium is preserved in congestive heart failure (CHF), the inotropic responsiveness to this compound should be preserved in CHF, and...

We aimed to characterize the relaxation induced by the soluble guanylyl cyclase (sGC) stimulator 5-cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-yl]pyrimidin-4-ylamine (BAY 41-2272) and its pharmacological interactions with nitric oxide (NO) in the corpus cavernosum (CC) from wild-type (WT), endothelial nitric-oxide synthase (eNOS)(-/-), and neuronal (n)NOS(-/-) mice. The effec...

Name Ronda R. Henning Margaret Knepper Kevin L. Fox Address Harris Corporation Government Communications Systems Division P.O. Box 37 Mail Stop W2/9703 Palm Bay, FL 32905 Harris Corporation Government Communications Systems Division P.O. Box 37 Mail Stop 2/9450 Palm Bay, FL 32905 Harris Corporation Government Communications Systems Division P.O. Box 37 Mail Stop 2/9450 Palm Bay, FL 32905 Phone ...

NOTE – NMFS is in the process of writing individual stock assessment reports for each of the 32 bay, sound and estuary stocks of bottlenose dolphins that are included in this report. Until this effort is completed and this report is replaced by 32 individual reports, basic information for all individual bay, sound and estuary stocks will remain in this report: “Northern Gulf of Mexico Bay, Soun...

BACKGROUND AND PURPOSE In endothelial dysfunction, signalling by nitric oxide (NO) is impaired because of the oxidation and subsequent loss of the soluble guanylyl cyclase (sGC) haem. The sGC activator 4-[((4-carboxybutyl){2-[(4-phenethylbenzyl)oxy]phenethyl}amino)methyl[benzoic]acid (BAY 58-2667) is a haem-mimetic able to bind with high affinity to sGC when the native haem (the NO binding site...

Bay k 8644 is a structural analog of nifedipine with positive inotropic activity. The mechanism of drug action was evaluated by measuring the effects of Bay k 8644 on twitch tension, action potential configuration, and calcium channel currents in myocardial cells. Bay k 8644 increases twitch tension in guinea pig atria without changing the time course of tension development. The drug does not o...

(-)-(R)-3-(2-Hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate (BAY 38-7271) is a new high-affinity cannabinoid receptor subtype 1 (CB1 receptor) ligand (K(i) = 0.46-1.85 nM; rat brain, human cortex, or recombinant human CB1 receptor), structurally unrelated to any cannabinoid receptor ligand known so far. BAY 38-7271 was characterized as a CB1 receptor agonist in 5-[gamma(35)S]-thi...

AIM The aim of the study was to evaluate the effect of BAY 11-7082, an NF-κB inhibitor, on basal and ET-1-induced production of reactive oxygen species (ROS), TNF-α and p65 protein in rat kidney. MATERIAL/METHODS The experimental animals were divided into five groups (n=7) receiving: 1) saline (control); 2 and 3) ET-1 in a dose of 3 μg/kg body weight (b.w.) or 12.5 μg/kg b.w.; 4) BAY 11-7082 ...