During the past two decades, enormous changes occurred in the management of gastric acid-related diseases. First, the histamine2-receptor antagonists were introduced, offering patients the first single-agent therapy that effectively reduced gastric acid secretion. Proton pump inhibitors became widely available in the early 1990s, and they generally appeared to be superior to the histamine2-rece...

Inhibition of the renin-angiotensin-aldosterone system (RAAS) is a key strategy in treating hypertension and cardiovascular and renal diseases. However, RAAS inhibitors (angiotensin-converting enzyme inhibitors, angiotensin receptor blockers, aldosterone receptor antagonists, and direct renin inhibitors) increase the risk of hyperkalemia (serum potassium >5.5 mmol/L). This review evaluates the ...

Platelet activation by thrombin plays a critical role in hemostasis and thrombosis. Based on structure-activity studies of a cloned platelet thrombin receptor, we designed two "mirror image" antagonists of thrombin and thrombin receptor function. First, "uncleavable" peptides mimicking the receptor domain postulated to interact with thrombin were found to be potent thrombin inhibitors. Second, ...

Background: IGF-1 and certain other cytokines have been shown to exert inflammatory/anti-inflammatory roles in chronic joint diseases. Objective: To assess the effect of IGF-1, IL-27 and IL-35, their interaction and their receptor expression in a rheumatoid arthritis model. Methods: Freund’s adjuvant-induced chronic joint inflammation was operated on 160 male rats. Animals were divided into his...

background: cellulite is the accumulation of subcutaneous fat and connective tissue in tights and buttocks. xanthines, such as aminophylline, are used as phosphodiesterase inhibitors, and are also adenosine receptor antagonists. objectives: the aim of the present study was to characterize in vitro aminophylline transdermal absorption through shed snake skin, and to investigate the absorption en...

Enantiomeric propanolamines have been identified as a new class of NR2B-selective NMDA receptor antagonists. The most effective agents are biaryl structures, synthesized in six steps with overall yields ranging from 11-64%. The compounds are potent and selective inhibitors of NR2B-containing recombinant NMDA receptors with IC 50 values between 30-100 nM. Potency is strongly controlled by substi...

The development of the direct oral anticoagulants (DOACs) represents one of the major breakthroughs in modern medicine over the last decade. Compared to vitamin K antagonists, all DOACs (dabigatran as a thrombin-Inhibitor, rivaroxaban, apixaban and edoxaban as factor Xa inhibitors) are much easier to handle due to their pharmacological properties. All DOACS are more efficacious and safer as vit...

Introduction Dysfunction in the brain serotonergic (5-HT) system is thought to underlie human depression. Selective Serotonin Re-uptake Inhibitors (SSRIs) are widely used antidepressant drugs whose therapeutic onset are delayed for several weeks whilst neuroadaptive changes take place in the brain, after which the previously disturbed serotonergic neurotransmission is restored. A suggested way ...

conclusions the application of 5-ht1a, 5-ht2, 5-ht3, 5-ht4, 5-ht6 and 5-ht7 receptor antagonists, applied at concentrations lower than 1.0 µm did not modify the efs-induced contraction and relaxation responses, whichsuggests the unlikely involvement of endogenous 5-ht in mediating responses to efs in the described test conditions. materials and methods segments taken from the rat duodenum, jeju...

BACKGROUND Placebo-controlled clinical trials have led to concern over possible increased risk of suicide-related events in some populations exposed to antidepressants. AIMS To evaluate the risk of suicide attempts by antidepressant drug class and the presence or absence of depression. METHOD A retrospective propensity-matched new-user cohort study was used to compare participants with inci...