Background and Purpose ?-Arrestin2 recruitment to ?-receptors may contribute the development of opioid side effects. This possibility led TRV130 PZM21, opioids reportedly biased against ?-arrestin2 in favour G-protein signalling. However, low efficacy by PZM21 simply reflect partial agonism overlooked due overexpression ?-receptors. Experimental Approach Efficacies apparent potencies DAMGO, mor...

We characterized a new iodinated, high affinity, linear V1a vasopressin antagonist, phenylacetylD-Tyr(Et)Phe-Gln-Asn-Lys-Pro-Arg-Tyr-NH2. The antagonist bound specifically to the V1a vasopressin receptor in crude rat liver membranes with an apparent Kd value of 0.168 nM. This affinity is approximately 1 order of magnitude greater than that of the natural agonist, vasopressin. The inhibitory act...

Foundational therapy for heart failure and a reduced ejection fraction consists of combination an angiotensin receptor–neprilysin inhibitor, beta-blocker, mineralocorticoid receptor antagonist sodium–glucose co-transporter 2 (SGLT2) inhibitor. However, the conventional approach to implementation is based on historically-driven sequence that not strongly evidence-based, typically requires ?6 mon...

this study was designed to investigate the role of gabab receptor agents on imipramine-induced antinociception in ligated and non-ligated mice using hot-plate test. the data showed that different doses of morphine (3, 6, and 9 mg/kg) induced a dose-dependent antinociception in ligated and non-ligated mice. however, the opioid response was decreased in ligated animals. intracerebroventricular (i...

objective(s) the central nucleus of the amygdala (cea) is a forebrain structure which is important in regulation of ingestive behavior and there is direct and circumstantial evidence to indicate that some circuits involved with feeding behavior include glutamatergic elements. the present study examined whether administration of nma (n-methyl-dl-aspartic acid) or mk801 into the cea altered water...

urokinase plasminogen activator receptor (upar) and its ligands play a major role in many tumors by mediating extracellular matrix degradation and signaling cascades leading to tumor growth, invasion and metastasis. recently we introduced upar decapeptide antagonist with cytotoxic effect on mda-mb-231 cell line. in this study we assessed the alteration in upar downstream signaling following tre...

Introduction: Previous studies have shown that the cannabinoid system is involved in anxiety.In addition, transient receptor potential vanilloid type-1 (TRPV1) channels are new targets for the development of anxiolytics. The present study investigated the possible interaction between the cannabinoid and vanilloid systems on anxiety-like behavior in rats. Methods: Four different groups of male ...

Adult-onset Still’s disease (AOSD) is a systemic autoinflammatory mediated by interleukin (IL)-1 production. There are no treatment guidelines for AOSD due to its rarity and heterogenous manifestations. Therefore, each case challenging requires multidisciplinary approach. We report of occurring in pregnant patient who did not respond standard with glucocorticoids developed skin reaction IL-1 re...

background: the ventral tegmental area (vta) is well known for its role in cardiovascular control. it is demonstrated that about 20-30% of the vta neurons are gabaergic though their role in cardiovascular control is not yet understood. this study is carried out to find the effects of gaba a and gaba b receptors on cardiovascular response of the vta. methods: experiments were performed on uretha...