Discovery of 2-(2-Chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a Novel, Bicyclic Lactam-Based Cannabinoid-1 Receptor Antagonist for the Treatment of Obesity

2009 ◽  
Vol 52 (9) ◽  
pp. 2652-2655 ◽  
Author(s):  
Robert L. Dow ◽  
Philip A. Carpino ◽  
John R. Hadcock ◽  
Shawn C. Black ◽  
Philip A. Iredale ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Cannabinoid 1 Receptor ◽  
Treatment Of Obesity

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

scholarly journals Cannabinoid-1 receptor antagonist rimonabant (SR141716) increases striatal dopamine D2 receptor availability

2011 ◽  
Vol 18 (6) ◽  
pp. 908-911 ◽  
Author(s):  
Cleo L. Crunelle ◽  
Elsmarieke van de Giessen ◽  
Sybille Schulz ◽  
Louk J. M. J. Vanderschuren ◽  
Kora de Bruin ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Striatal Dopamine ◽  
Dopamine D2 ◽  
Cannabinoid 1 Receptor

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

scholarly journals Spinal Cannabinoid Receptor Type 2 Activation Reduces Hypersensitivity and Spinal Cord Glial Activation after Paw Incision

2007 ◽  
Vol 106 (4) ◽  
pp. 787-794 ◽  
Author(s):  
Alfonso Romero-Sandoval ◽  
James C. Eisenach
Keyword(s):  
Spinal Cord ◽  
Side Effects ◽  
Receptor Antagonist ◽  
Cannabinoid Receptors ◽  
Cannabinoid Receptor ◽  
Intrathecal Injection ◽  
Intrathecal Administration ◽  
Glial Activation ◽  
Receptor Agonists ◽  
Cannabinoid 1 Receptor

Background Cannabinoids bind to cannabinoid receptors type 1 and 2 and produce analgesia in several pain models, but central side effects from cannabinoid 1 receptors limit their clinical use. Cannabinoid 2 receptors reduce inflammatory responses in the periphery by acting on immune cells, and they are present on glia in the central nervous system. This study tested whether spinal cannabinoid activation would induce analgesia, glial inhibition, and central side effects in a postoperative model or incisional pain. Methods Rats underwent paw incision surgery, with intrathecal injections of cannabinoid agonists and antagonists and assessment of withdrawal thresholds and behavioral side effects. Spinal glial activation was determined by immunohistochemistry. Results Intrathecal administration CP55940 reduced postoperative hypersensitivity (91 +/- 9% maximum possible effect; P < 0.05), and this was prevented by intrathecal administration of both cannabinoid 1 receptor (AM281) and cannabinoid 2 receptor (AM630) antagonists. CP55940 also caused several behavioral side effects, and these were prevented by the cannabinoid 1 receptor but not by the cannabinoid 2 receptor antagonist. Intrathecal injection of the cannabinoid 2 receptor agonist JWH015 reversed postoperative hypersensitivity (89 +/- 5% maximum possible effect; P < 0.05), and this was reversed by the cannabinoid 2 but not by the cannabinoid 1 receptor antagonist. JWH015, which did not induce behavioral side effects, reduced paw incision induced microglial and astrocytic activation in spinal cord (P < 0.05). Conclusions These data indicate that intrathecal administration of cannabinoid receptor agonists may provide postoperative analgesia while reducing spinal glial activation, and that selective cannabinoid 2 receptor agonists may do so without central side effects.

Characterization of AJ5012 as a Novel Peripheral Cannabinoid 1 Receptor Antagonist in Mouse Models of Obesity

Diabetes ◽  
2018 ◽  
Vol 67 (Supplement 1) ◽  
pp. 2026-P
Author(s):  
JUNGEUN KIM ◽  
JUHWAN YOON ◽  
EUNHA KIM ◽  
SUNG-HWA YOON ◽  
WOOK KIM
Keyword(s):  
Receptor Antagonist ◽  
Mouse Models ◽  
Cannabinoid 1 Receptor
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