Vasopressin receptor antagonists are a new class of drugs that address the problems of fluid retention, hyponatremia, and renal dysfunction in heart failure. Elevated vasopressin levels in heart failure cause myocardial fibrosis, hypertrophy and vasoconstriction by activating the V1a receptors, as well as water retention and hyponatremia by activating V2 receptors. Antagonism of V1a receptors a...

The biochemical and pharmacological profile of YM087, 4'-[(2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepin- 6-yl)-carbonyl]-2-phenylbenzanilide monohydrochloride, a newly synthesized nonpeptide vasopressin (AVP) antagonist, was investigated in several in vitro and in vivo studies. YM087 showed high affinity for V1A receptors from rat liver and V2 receptors from rat kidney with Ki values ...

The vasopressin receptor 2 (V2) receptor antagonist tolvaptan is an aquaretic agent that has been found to improve symptoms in patients with congestive heart failure. In this study (SMILE study), we administered tolvaptan to patients aged ≥ 80 years with heart failure accompanied by congestive symptoms and compared its effectiveness and safety profiles in this group with those in patients < 80 ...

Normal aging is associated with vasopressin neuron adaptation, but little is known about its effects on the release of apelin, an aquaretic peptide colocalized with vasopressin. We found that plasma vasopressin concentrations were higher and plasma apelin concentrations lower in aged rats than in younger adults. The response of AVP/apelin neurons to osmotic challenge was impaired in aged rats. ...

The present study was performed to investigate the renal handling of water in rats with decompensated liver cirrhosis. Liver cirrhosis was induced by intraperitoneal administration of carbon tetrachloride twice weekly for 16 wk. Control rats were treated with vehicle. The cirrhotic rats developed severe disturbances in water homeostasis: urine production was decreased and hyperosmotic, the rats...

fractions obtained from partitioning of aerial methanolic extract of euphorbia aellenii with chloroform (e2), ethyl acetate (e3), n-butanol (e4) and water (e5) were investigated in vitro for their phytotoxicity, insecticidal, anti-leishmanial, cytotoxicity, antibacterial and antifungal activities. sample e2 appeared to have significant phytotoxic activity. in the insecticidal screening study on...

abstract: in a wide search program towards new and efficient antimicrobial agents, a series of 4-substituted-1,2,4-triazolidine-3,5-dione derivatives namely urazoles holding an alkyl moiety at position 4 have been synthesized and tested for their in vitro antibacterial and antifungal activities. the structures of these compounds have been investigated by spectral data. the synthesized compounds...

PURPOSE OF REVIEW Portal hypertension is responsible for most of the complications associated with cirrhosis, specifically variceal hemorrhage, ascites and hepatic encephalopathy. Progress in understanding the pathophysiology of portal hypertension and improvements in the diagnosis and management of its complications that have occurred over the last year are discussed. RECENT FINDINGS Endothe...