Several clinical studies have investigated the potential benefits of endothelin receptor antagonism in chronic pathologies such as diabetic kidney disease. However, fluid retention and edema have been identified as major side effects of endothelin receptor antagonists. In the present study we hypothesized that avosentan which was described as a predominant ET(A) receptor antagonist would produc...

RES-1149-1 and -2, novel and non-peptidic endothelin antagonists, were isolated from the cultured broth of a fungus, Aspergillus sp. RE-1 149. RES-1 149-1 and -2 selectively inhibited the ET-1 binding to endothelin type B receptor (ETB receptor) with IC50 values of 1.5pM and 20//M, respectively. Taxonomyof producing strains, fermentation, isolation, and physico-chemical properties of RES-1149-1...

An impairment of cardiac norepinephrine (NE) reuptake via the neuronal NE transporter (NET) enhances the effects of increased cardiac NE release in heart failure patients. Increasing evidence suggests that aldosterone and endothelins promote sympathetic overstimulation of failing hearts. Salt-sensitive Dahl rats (DS) fed a high-salt diet developed arterial hypertension and diastolic heart failu...

Immunoreactive endothelin 1 (irET-1) concentrations were measured in extracts prepared from 4 phyllodes tumors and 14 fibroadenomas. irET-1 was detectable in all tissue extracts by specific radioimmunoassay, and the mean concentration of irET-1 was 18-fold and 27-fold higher in tissue extracts from phyllodes tumors than in those from intracanalicular fibroadenomas and pericanalicular fibroadeno...

the aim of the present study was to investigate whether and by which mechanism; histamine can induce state-dependent retrieval of passive avoidance task. the pre-training or pre-test intracerebroventricular (i.c.v.) injection of histamine (20µg/mouse) impaired retrieval, when it was tested 24 h later. in the animals, which retrieval was impaired due to histamine pre-training administration, pre...

background and objective: host genetic factors such as cytokine gene polymorphisms as well as helicobacter pylori (h. pylori) infection have been found to be associated with gastric cancer risk . interleukin 1 is a pro-inflammatory cytokine involved in h. pylori-induced gastric inflammation. therefore, we analyzed the association between il-1β and il-1-rn polymorphisms and gastric cancer in per...

S ince its discovery in 1988 [1], the role of endothelin in cardiovascular disease has been intensively studied. Activation of the endothelin system is considered part of the neurohormonal response in congestive heart failure. Endothelin is produced by vascular endothelial cells and has potent vasoconstrictor effects [2]. Elevated endothelin levels induce adverse cardiac remodelling and cause p...