Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists

2009 ◽  
Vol 19 (17) ◽  
pp. 5195-5199 ◽  
Author(s):  
Wu Du ◽  
James P. Jewell ◽  
Linus S. Lin ◽  
Vincent J. Colandrea ◽  
Jing C. Xiao ◽  
...  
Keyword(s):  
Inverse Agonists ◽  
Cannabinoid 1 Receptor

1-Sulfonyl-4-acylpiperazines as Selective Cannabinoid-1 Receptor (CB1R) Inverse Agonists for the Treatment of Obesity

2009 ◽  
Vol 52 (8) ◽  
pp. 2550-2558 ◽  
Author(s):  
Petr Vachal ◽  
Joan M. Fletcher ◽  
Tung M. Fong ◽  
Cathy C. R.-R. Huang ◽  
Julie Lao ◽  
...  
Keyword(s):  
Inverse Agonists ◽  
Cannabinoid 1 Receptor ◽  
Treatment Of Obesity

Synthesis and Evaluation of Dibenzothiazepines: A Novel Class of Selective Cannabinoid-1 Receptor Inverse Agonists

2009 ◽  
Vol 52 (7) ◽  
pp. 1975-1982 ◽  
Author(s):  
Hanna Pettersson ◽  
Anne Bülow ◽  
Fredrik Ek ◽  
Jacob Jensen ◽  
Lars K. Ottesen ◽  
...  
Keyword(s):  
Inverse Agonists ◽  
Cannabinoid 1 Receptor

Benzodioxoles: Novel Cannabinoid-1 Receptor Inverse Agonists for the Treatment of Obesity

2008 ◽  
Vol 51 (7) ◽  
pp. 2115-2127 ◽  
Author(s):  
Leo Alig ◽  
Jochem Alsenz ◽  
Mirjana Andjelkovic ◽  
Stefanie Bendels ◽  
Agnès Bénardeau ◽  
...  
Keyword(s):  
Inverse Agonists ◽  
Cannabinoid 1 Receptor ◽  
Treatment Of Obesity

Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists

2007 ◽  
Vol 17 (8) ◽  
pp. 2184-2187 ◽  
Author(s):  
Helen E. Armstrong ◽  
Amy Galka ◽  
Linus S. Lin ◽  
Thomas J. Lanza ◽  
James P. Jewell ◽  
...  
Keyword(s):  
Inverse Agonists ◽  
Cannabinoid 1 Receptor

Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation. Part 1

2010 ◽  
Vol 20 (4) ◽  
pp. 1448-1452 ◽  
Author(s):  
John S. Debenham ◽  
Christina B. Madsen-Duggan ◽  
Richard B. Toupence ◽  
Thomas F. Walsh ◽  
Junying Wang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Inverse Agonists ◽  
Cannabinoid 1 Receptor ◽  
Synthesis And Biological Evaluation

Pharmacophore and 3D-QSAR Studies on 1-Sulfonyl-4-acylpiperazines as Selective Cannabinoid-1 Receptor (CB1R) Inverse Agonists

2011 ◽  
Vol 8 (7) ◽  
pp. 659-670
Author(s):  
Vikas N. Telvekar ◽  
Lalit B. Thakur ◽  
Prashant B. Jagdhane ◽  
Yogesh D. Manohar
Keyword(s):  
3D Qsar ◽  
Inverse Agonists ◽  
Qsar Studies ◽  
Cannabinoid 1 Receptor

scholarly journals Gastrointestinal Adverse Events of Cannabinoid 1 Receptor Inverse Agonists suggest their Potential Use in Irritable Bowel Syndrome with Constipation: A Systematic Review and Meta-Analysis

2019 ◽  
Vol 28 (4) ◽  
pp. 473-481 ◽  
Author(s):  
Adam Fabisiak ◽  
Marcin Włodarczyk ◽  
Natalia Fabisiak ◽  
Martin Storr ◽  
Jakub Fichna
Keyword(s):  
Clinical Trials ◽  
Irritable Bowel Syndrome ◽  
Adverse Events ◽  
Therapeutic Option ◽  
Meta Analysis ◽  
Endocannabinoid System ◽  
Inverse Agonists ◽  
Cannabinoid 1 Receptor ◽  
Irritable Bowel ◽  
Potential Use

Background and Aims: Irritable bowel syndrome (IBS) is one of the most common functional gastrointestinal (GI) disorders characterized by pain and impaired bowel movements. Currently available drugs show limited efficacy. Cannabinoid 1 receptor (CB1) inverse agonists (CB1-RAN) cause diarrhea and may be candidates for the treatment of constipation-predominant IBS (IBS-C). We evaluated the effects of CB1-RAN in clinical trials for their potential use in IBS-C. Methods: Database search identified all clinical trials published up to May 2018 that reported rimonabant and taranabant treatment for at least one month and detailed the GI adverse events (AEs). Categorical outcomes (subgroups of AEs) were analyzed using the odds ratio (OR). Results: Eighteen trials met the inclusion criteria. Rimonabant 20 mg produced significantly more overall AEs (OR=1.35, CI: 1.19–1.52, p<0.0001), psychiatric events (OR=1.79, CI: 1.46–2.21, p<0.001) and GI AEs (OR=2.05, CI: 1.65–2.55, p<0.001) compared to placebo. Taranabant at doses ranging from 0.5 to 8 mg produced significantly more overall AEs (OR=1.36, CI: 1.13-1.64, p<0.002), psychiatric AEs (1.82, CI: 1.54–2.16, p<0.001) and GI AEs (OR=1.75, CI: 1.29–2.37, p<0.001) compared to placebo. Conclusions: The approach to target CB1 in the gut for the treatment of IBS-C or chronic constipation seems a promising therapeutic option. Prospective clinical trials on the possible targeting of CB1 and the endocannabinoid system are warranted.

Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation

2009 ◽  
Vol 19 (9) ◽  
pp. 2591-2594 ◽  
Author(s):  
John S. Debenham ◽  
Christina B. Madsen-Duggan ◽  
Junying Wang ◽  
Xinchun Tong ◽  
Julie Lao ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Inverse Agonists ◽  
Cannabinoid 1 Receptor ◽  
Synthesis And Biological Evaluation
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