the effects of chronic stress and glucocorticoids receptor antagonist (ru486) on expression of melanocortin 4 receptor (mc4r) mrna in arcuate nucleus (arc) of male rats were evaluated. in this study, adult male sprague dawley rats were placed into four groups (n=6/group) stress, ru486, stress/ru486, and control groups. in stress group, the rats were restrained, 1 h/day, for 12 days. in ru486 gr...

Abstract The leptin-melanocortin pathway is playing a pivotal role for central body weight regulation. melanocortin 4 receptor (MC4R) essential to induce satiety after activation by the endogenous ligands α-/β-melanocyte-stimulating hormone. relevance of biased signaling exemplified an MC4R agonist, which has been approved treatment rare forms monogenic obesity. Here discussed as new option dev...

despite a quite short early history, computational drug design and discovery methods can now be efficient in reducing costs and speeding up drug developing procedure. melanocortin-4 receptor (mc4r) is a g protein-coupled receptor implicated in the regulation of body weight. despite its clinical reputation, there is a lack of in-depth knowledge about structure and behavior of mc4r in lipid bilay...

Agouti-related protein (AGRP) is an endogenous antagonist of melanocortin action that functions in the hypothalamic control of feeding behavior. Although previous studies have shown that AGRP binds three of the five known subtypes of melanocortin receptor, the receptor domains participating in binding and the molecular interactions involved are presently unknown. The present studies were design...

objective: melanocortin-4 receptor (mc4r) and agouti-related peptide (agrp) are involved in energy homeostasis in the rat. the aim of the present study was to evaluate the expression of mc4r and agrp mrnas in arcuate nucleus (arc) during long term malnutrition of female ovariectomized rats. materials and methods: ten female ovariectomized rats were divided into two equal groups (n=6) of normal ...

Haploinsufficiency of the melanocortin-4 receptor, the most common monogenetic obesity syndrome in humans, is associated with a reduction in autonomic tone, bradycardia, and incidence of obesity-associated hypertension. Thus, it has been assumed that melanocortin obesity syndrome may be protective with respect to obesity-associated cardiovascular disease. We show here that absence of the melano...

The melanocortin system is a critical component of the forebrain and hindbrain regulatory systems involved in energy balance. This system is composed of pro-opiomelanocortin (POMC) neurons that act, in part, through the melanocortin-4 receptor (MC4R). Although the importance of the melanocortin system in controlling feeding has been established for two decades, the understanding of the developm...

The effects of chronic stress and glucocorticoids receptor antagonist (RU486) on expression of melanocortin 4 receptor (MC4R) mRNA in arcuate nucleus (ARC) of male rats were evaluated. In this study, adult male Sprague Dawley rats were placed into four groups (n=6/group) stress, RU486, stress/RU486, and control groups. In stress group, the rats were restrained, 1 h/day, for 12 days. In RU486 gr...

The melanocortin 4 receptor (MC4R) is a G-protein coupled receptor mainly expressed in the central nervous system of vertebrates. Activation of the MC4R leads to a decrease in food intake, while inactivating mutations are a genetic cause of obesity. The binding of agoutirelated protein (AGRP) reduces agonist-stimulated cAMP production (competitive antagonist) but also the basal activity of the ...