Arginine-stimulated insulin and somatostatin release is enhanced by the sulfonylurea gliclazide. In contrast, gliclazide inhibits the glucagon response. The aim of the present study was to investigate whether this inhibition of glucagon release was mediated by a direct suppressive effect of gliclazide or was secondary to the paracrine effect of released somatostatin. To eliminate the paracrine ...

In the present study, interactions of dopamine receptor agonists and antagonists with water swimming stress (WSS) on naloxone-induced jumping in morphine-dependent mice were examined. Mice were rendered dependent as described in the methods section. The opioid receptor antagonist, naloxone (1 mg/kg), was injected to elicit jumping (as a withdrawal sign). The first group exposed to WSS in the pr...

objective(s): atherosclerosis is an important risk factor for coronary heart disease. neuropeptide y (npy) and its receptors, located in peripheral tissue such as white adipose tissue, have been linked to obesity and fat storage. the role of npy in atherosclerosis has not yet been fully studied, so this study was conducted to further investigate the effect of biie 0246, an npy receptor antagoni...

in the present study, interactions of dopamine receptor agonists and antagonists with water swimming stress (wss) on naloxone-induced jumping in morphine-dependent mice were examined. mice were rendered dependent as described in the methods section. the opioid receptor antagonist, naloxone (1 mg/kg), was injected to elicit jumping (as a withdrawal sign). the first group exposed to wss in the pr...

The amino acid 4-fluoro-L-phenylalanine (4F-Phe) was introduced at the positions of Phe6 and Phe22 in the 29-residue polypeptide hormone glucagon by expressing glucagon in E. coli in the presence of an excess of 4F-Phe. Glucagon regulates blood glucose homeostasis by interaction with the glucagon receptor (GCGR), a class B GPCR. By referencing to the 4F-Phe chemical shifts at varying D2O concen...

The present study sought to determine whether central glucagon-like peptide-1 (GLP-1)-receptor signalling contributes to the anorexigenic effects of systemically administered lithium chloride (LiCl). Male Sprague-Dawley rats with chronic intracerebroventricular (ICV) cannulas were acclimated to a feeding schedule that included daily 30-min access to palatable mash. In the first experiment, ICV ...

Receptor recognition by the Asp(3) residues of vasoactive intestinal peptide and secretin requires the presence of a lysine residue close to the second transmembrane helix (TM2)/first extracellular loop junction and an ionic bond with an arginine residue in TM2. We tested whether the glucagon Gln(3) residue recognizes the equivalent positions in its receptor. Our data revealed that the binding ...

this study was conducted to investigate the possible involvement of the histaminergic system in themediation of ghrelin-induced feeding behavior in broiler chickens. in the trial 1, the effect ofintracerebroventricular (icv) injection of ghrelin on feed intake was examined in 3-h feed-deprived broilerchickens. in the trials 2 and 3, the chickens were received icv chlorpheniramine (an h1 recepto...

GLP-1-(7-36)-amide and exendin-4-(1-39) are glucagon-like peptide-1 (GLP-1) receptor agonists, whereas exendin-(9-39) is the only known antagonist. To analyze the transition from agonist to antagonist and to identify the amino acid residues involved in ligand activation of the GLP-1 receptor, we used exendin analogs with successive N-terminal truncations. Chinese hamster ovary cells stably tran...

Abstract Objectives Peyronie’s disease (PD) is characterised by formation of a fibrotic plaque in the tunica albuginea which caused excessive myofibroblast presence and activity. A previous phenotypic screening campaign that tested 1,954 FDA-approved drugs for their ability to inhibit transformation PD-derived fibroblasts revealed 26 hits. Of these, we investigated following hits further; terfe...