Peripherally Selective CB1 Receptor Antagonist Improves Symptoms of Metabolic Syndrome in Mice

2021 ◽  
Vol 4 (2) ◽  
pp. 757-764
Author(s):  
Nayaab Khan ◽  
Lucas Laudermilk ◽  
Jalen Ware ◽  
Taylor Rosa ◽  
Kelly Mathews ◽  
...  
Keyword(s):  
Metabolic Syndrome ◽  
Receptor Antagonist ◽  
Cb1 Receptor ◽  
Cb1 Receptor Antagonist

scholarly journals Rimonabant: From RIO to Ban

2011 ◽  
Vol 2011 ◽  
pp. 1-4 ◽  
Author(s):  
Amir H. Sam ◽  
Victoria Salem ◽  
Mohammad A. Ghatei
Keyword(s):  
Metabolic Syndrome ◽  
Weight Loss ◽  
Side Effects ◽  
Receptor Antagonist ◽  
Mood Disorders ◽  
Cb1 Receptor ◽  
Phase 3 ◽  
Mass Market ◽  
The Metabolic Syndrome ◽  
Cb1 Receptor Antagonist

Endocannabinoid antagonism as a treatment for obesity and the metabolic syndrome became a hugely anticipated area of pharmacology at the start of the century. The CB1 receptor antagonist Rimonabant entered the European mass market on the back of several trials showing weight loss benefits alongside improvements in numerous other elements of the metabolic syndrome. However, the drug was quickly withdrawn due to the emergence of significant side effects—notably severe mood disorders. This paper provides a brief overview of the Rimonabant story and places the recent spate of FDA rejections of other centrally acting weight loss drugs entering Phase 3 trials in this context.

scholarly journals Monoacylglycerol lipase inhibition attenuates acute and anticipatory nausea in rats

SURG Journal ◽  
2014 ◽  
Vol 7 (3) ◽  
pp. 21-29
Author(s):  
Rachel I. Downey ◽  
Cheryl L. Limebeer ◽  
Heather I. Morris ◽  
Linda A. Parker
Keyword(s):  
Receptor Antagonist ◽  
Receptor Activation ◽  
Cb1 Receptor ◽  
Monoacylglycerol Lipase ◽  
Anticipatory Nausea ◽  
Acute Nausea ◽  
Sr 141716 ◽  
Cb1 Receptor Antagonist ◽  
Lipase Inhibition

This study investigates the role of the endocannabinoid 2-arachidonyl glycerol (2-AG) in regulating acute and anticipatory nausea in rats using the conditioned gaping model. The animals were systemically pretreated with MJN110, a selective monoacylglycerol lipase (MAGL) inhibitor, to enhance endogenous levels of 2-AG. Acute nausea was assessed using the taste reactivity model in which a flavour, saccharin, was paired with the administration of the emetic agent, lithium chloride (LiCl). Anticipatory nausea was assessed using a model of contextually elicited conditioned gaping in which a context was paired with the emetic agent, LiCl. Results indicated that MJN110 at the 10.0 mg kg-1 and 20.0 mg kg-1 dosage significantly attenuated acute and anticipatory nausea, as displayed by the significant reduction in mean number of gapes. This suppression was mediated by CB1 receptor activation as displayed by reversal of such effects when MJN110 was coadministered with the CB1 receptor antagonist, SR 141716. The results suggest that enhancement of endogenous 2-AG levels by MAGL inhibition may have anti-emetic potential. Keywords: 2-arachidonyl glycerol; monoacylglycerol lipase; endocannabinoid; nausea; conditioned gaping; CB1 receptor

scholarly journals Rimonabant, a Selective Cannabinoid CB1 Receptor Antagonist, Inhibits Atherosclerosis in LDL Receptor–Deficient Mice

2009 ◽  
Vol 29 (1) ◽  
pp. 12-18 ◽  
Author(s):  
Frédérique Dol-Gleizes ◽  
Réjane Paumelle ◽  
Virgile Visentin ◽  
Anne-Marie Marés ◽  
Perrine Desitter ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Ldl Receptor ◽  
Cb1 Receptor ◽  
Cannabinoid Cb1 Receptor ◽  
Cb1 Receptor Antagonist ◽  
Deficient Mice ◽  
Cannabinoid Cb1 Receptor Antagonist

scholarly journals Remote CB1 receptor antagonist administration reveals multiple sites of tonic and phasic endocannabinoid neuroendocrine regulation

2020 ◽  
Vol 113 ◽  
pp. 104549 ◽  
Author(s):  
R.J. Newsom ◽  
R.J. Garcia ◽  
J. Stafford ◽  
C. Osterlund ◽  
C.E. O’Neill ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Cb1 Receptor ◽  
Neuroendocrine Regulation ◽  
Cb1 Receptor Antagonist
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