Endocrine Abstracts

It is well known that cannabinoid type 1 receptor (CB1) antagonist drugs may reduce body weight and improve metabolic profiles in obese animals and humans by a double mechanism: at first, targeting mesolimbic and hypothalamic nuclei and, thereafter, peripheral organs involved in energy storage and expenditure. However, it is still unknown which of these sites of action may have a predominant role in the endocannabinoid effect on energy balance regulation. To solve this questio...

The endocannabinoid system has recently emerged as an important modulator of several functions of adipose tissue by altering cell proliferation and gene expression. In this work, we investigated the effects of CB1 activation/blockade in mouse 3T3-L1 adypocite cells by using WIN55,212, a CB1/CB2 agonist and rimonabant, a specific CB1 antagonist, in different experimental settings such as acute treatment on pre-adipocytes and on mature adipocytes, and chronic treatment during di...

Bile acids (BA) are cholesterol-derived molecules that are mostly known for their involvement in lipid digestion and absorption. Recent evidence recognizes them as metabolic integrators able to reduce body weight (BW), increase energy expenditure (EE) and improve glycemic control by activating their specific receptor, the Takeda G protein-coupled receptor 5 (TGR5) in peripheral organs. These outcomes have increased importance in the context of diet-induced obesity and associat...

Type 2 diabetes is among the most prevalent chronic diseases worldwide. Further research is needed to identify new mechanisms that may help preserve the function of insulin-secreting pancreatic β-cells. The cannabinoid receptors type 1 (CB1) and their endogenous ligands, endocannabinoids, exert a key role in regulating of glucose homeostasis, β-cells function, and insulin secretion. Intriguingly, CB1 is not only located at the plasma membrane (pmCB1), but also at the...

Obesity and type–2 diabetes (T2D) represent a global health crisis. However, only a few, and often sub–effective pharmacological tools are available to treat these disorders. Though beneficial for glycemic control, GLP–1 receptor (GLP–1R) agonists show scarce weight–lowering and insulin–sensitizing efficacy.New molecules able to selectively block the activity of the cannabinoid receptor type–1 (CB1R) in periphera...

The pharmacological blockade of cannabinoid receptor type 1 (CB1) has been shown to counteract diet induced obesity (DIO). An unsolved question is whether the effects of CB1 blockade on energy balance are due to peripheral or central mechanisms. This is an important clinical issue since the CB1 antagonist drugs have recently been withdrawn from the market due to their psychiatric side effects, and novel drugs selectively acting at peripheral le...

Aims: Recently, the endocannabinoid system emerged as a pivotal regulator of food intake, ingestive behavior and energy metabolism, acting through CB1 and its endogenous ligands, the endocannabinoids. CB1 antagonists may reduce body weight and improve metabolic profiles in animals and humans by a double mechanism: at first, they target mesolimbic and hypothalamic nuclei and, thereafter, peripheral organs involved in energy storage and expenditure. Nevertheless, it is still unk...