a series of angiotensin ii (a ii) receptor antagonist of some substituted 5-(biphenyl-4-ylmethyl) pyrazole were subjected to qsar analysis using hansch and fujita-ban model, by using combination of thermodynamic, electronic, spatial descriptor and presence or absence of substituent respectively. several qsar model were obtained using stepwise regression analysis. two models from both the method...

Selective Endothelin Receptor Involvement in the Development of Colorectal Cancer and Liver Metastases Endothelin-1 (ET-1), a vasoactive peptide with mitogenic qualities, is over­ expressed in the plasma of patients with colorectal cancer (CRC) and liver metastases. Its actions are mediated via two G-protein linked receptors, ETA and ETb. This study (i) examined the effect of ET-1 and its recep...

Adrenomedullin, originally discovered in human pheochromocytoma, is a vasodilating and natriuretic peptide of vascular endothelial and smooth muscle cell origin. Although endothelin-1 (ET-1) has been implicated as a vasoconstricting and growth-promoting peptide of endothelial origin, it may more importantly function as an autocrine factor and release vasodilatory substances such as nitric oxide...

Since the discovery of ET-1 in 1988 [1], few molecules have come under such intense scrutiny as the endothelin peptide family (ET-1, ET-2, ET-3) and their receptors (ETA, ETB, ETC). Much study had nevertheless given rise to, at best, a limited understanding of their regulation and roles in health and disease. Perhaps it was not surprising that 'endothelin fatigue' had begun to sink in, even amo...

Policy Blue Cross and Blue Shield of Kansas City will provide coverage for the pharmacologic treatment of pulmonary arterial hypertension (PAH) with prostacyclin analogues, endothelin receptor antagonists, or phosphodiesterase type 5 (PDE5) inhibitors when it is determined to be medically necessary because the following criteria are met. Conventional pharmacologic therapies are considered in al...

Pulmonary arterial hypertension (PAH) is a fatal disease associated with vasoconstriction and vascular remodelling. There are three well-known pathways that contribute to the pathogenesis of PAH: endothelin, nitric oxide and prostacyclin. Treatments targeting these pathways are well established in clinical practice, such as endothelin receptor antagonists, phosphodiesterase type-5 inhibitors an...

objective: argemone mexicana is a papaveracea plant; some reports have shown their antibacterial, anti-cancer, sedative and probably anti-anxiety properties. from their aerial parts, flavonoids and alkaloids have been isolated, which are intrinsically related to some actions on the central nervous system. the aim of this study was to evaluate the anxiolytic-like effects of the plant, using its ...

BACKGROUND Endothelin-1 is a potent endogenous vasoconstrictor that contributes to renal microcirculatory impairment during endotoxemia and sepsis. Here we investigated if the renal circulatory and metabolic effects of endothelin during endotoxemia are mediated through activation of endothelin-A receptors. METHODS AND FINDINGS A randomized experimental study was performed with anesthetized an...

In the present study, the effects of different doses of nicotine on immobility time in mice were tested. Intraperitioneal administration of low doses of nicotine (0.025 mg/kg) decreased, but higher doses (0.8 and 1 mg/kg) increased immobility time. The anti-immobility response induced by low doses of nicotine was inhibited by high doses of the D2 receptor antagonist sulpiride, the central nicot...