CB1Cannabinoid Receptor Antagonists for Treatment of Obesity and Prevention of Comorbid Metabolic Disorders

2006 ◽  
Vol 49 (14) ◽  
pp. 4008-4016 ◽  
Author(s):  
Jochen Antel ◽  
Peter C. Gregory ◽  
Ulrich Nordheim
Keyword(s):  
Metabolic Disorders ◽  
Receptor Antagonists ◽  
Treatment Of Obesity

scholarly journals AMPK as a mediator of hormonal signalling

2009 ◽  
Vol 44 (2) ◽  
pp. 87-97 ◽  
Author(s):  
Chung Thong Lim ◽  
Blerina Kola ◽  
Márta Korbonits
Keyword(s):  
Protein Synthesis ◽  
Fatty Acid ◽  
Metabolic Disorders ◽  
Energy Homeostasis ◽  
Metabolic Effects ◽  
Whole Body ◽  
Acid Oxidation ◽  
Treatment Of Obesity ◽  
Amp Activated Protein Kinase ◽  
Hormonal Signalling

AMP-activated protein kinase (AMPK) is a key molecular player in energy homeostasis at both cellular and whole-body levels. AMPK has been shown to mediate the metabolic effects of hormones such as leptin, ghrelin, adiponectin, glucocorticoids and insulin as well as cannabinoids. Generally, activated AMPK stimulates catabolic pathways (glycolysis, fatty acid oxidation and mitochondrial biogenesis) and inhibits anabolic pathways (gluconeogenesis, glycogen, fatty acid and protein synthesis), and has a direct appetite-regulating effect in the hypothalamus. Drugs that activate AMPK, namely metformin and thiazolidinediones, are often used to treat metabolic disorders. Thus, AMPK is now recognised as a potential target for the treatment of obesity and associated co-morbidities.

Synthesis and Evaluation of New Arylsulfonamidomethylcyclohexyl Derivatives as Human Neuropeptide Y Y5 Receptor Antagonists for the Treatment of Obesity.

ChemInform ◽  
2004 ◽  
Vol 35 (30) ◽  
Author(s):  
Antonio Moreno ◽  
Silvia Perez ◽  
Silvia Galiano ◽  
Laura Juanenea ◽  
Oihana Erviti ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Treatment Of Obesity

scholarly journals Angiotensin AT1 receptor antagonism by losartan stimulates adipocyte browning via induction of apelin

2020 ◽  
Vol 295 (44) ◽  
pp. 14878-14892
Author(s):  
Dong Young Kim ◽  
Mi Jin Choi ◽  
Tae Kyung Ko ◽  
Na Hyun Lee ◽  
Ok-Hee Kim ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Protein Kinase ◽  
Metabolic Disorders ◽  
Angiotensin Ii Receptor ◽  
Adeno Associated Virus ◽  
Receptor Antagonism ◽  
White Adipocytes ◽  
Treatment Of Obesity ◽  
Amp Activated Protein Kinase

Adipocyte browning appears to be a potential therapeutic strategy to combat obesity and related metabolic disorders. Recent studies have shown that apelin, an adipokine, stimulates adipocyte browning and has negative cross-talk with angiotensin II receptor type 1 (AT1 receptor) signaling. Here, we report that losartan, a selective AT1 receptor antagonist, induces browning, as evidenced by an increase in browning marker expression, mitochondrial biogenesis, and oxygen consumption in murine adipocytes. In parallel, losartan up-regulated apelin expression, concomitant with increased phosphorylation of protein kinase B and AMP-activated protein kinase. However, the siRNA-mediated knockdown of apelin expression attenuated losartan-induced browning. Angiotensin II cotreatment also inhibited losartan-induced browning, suggesting that AT1 receptor antagonism-induced activation of apelin signaling may be responsible for adipocyte browning induced by losartan. The in vivo browning effects of losartan were confirmed using both C57BL/6J and ob/ob mice. Furthermore, in vivo apelin knockdown by adeno-associated virus carrying–apelin shRNA significantly inhibited losartan-induced adipocyte browning. In summary, these data suggested that AT1 receptor antagonism by losartan promotes the browning of white adipocytes via the induction of apelin expression. Therefore, apelin modulation may be an effective strategy for the treatment of obesity and its related metabolic disorders.

Discovery of a promising agent IQZ23 for the treatment of obesity and related metabolic disorders

2020 ◽  
Vol 192 ◽  
pp. 112172
Author(s):  
Yong Rao ◽  
Zhao Xu ◽  
Yu-Tao Hu ◽  
Chan Li ◽  
Yao-Hao Xu ◽  
...  
Keyword(s):  
Metabolic Disorders ◽  
Promising Agent ◽  
Treatment Of Obesity

Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity

2007 ◽  
Vol 17 (10) ◽  
pp. 2706-2711 ◽  
Author(s):  
Roger A. Smith ◽  
Zahra Fathi ◽  
Furahi Achebe ◽  
Christiana Akuche ◽  
Su-Ellen Brown ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Cannabinoid 1 Receptor ◽  
Amide Derivatives ◽  
Treatment Of Obesity
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