Recent CB1 cannabinoid receptor antagonists and inverse agonists

2009 ◽  
Vol 70 (8) ◽  
pp. 601-615 ◽  
Author(s):  
Herbert H. Seltzman
Keyword(s):  
Cannabinoid Receptor ◽  
Receptor Antagonists ◽  
Inverse Agonists ◽  
Cb1 Cannabinoid Receptor

Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists

2009 ◽  
Vol 17 (7) ◽  
pp. 2842-2851 ◽  
Author(s):  
Andrea Behrenswerth ◽  
Nicole Volz ◽  
Jakob Toräng ◽  
Sonja Hinz ◽  
Stefan Bräse ◽  
...  
Keyword(s):  
Cannabinoid Receptor ◽  
Coumarin Derivatives ◽  
Receptor Antagonists ◽  
Inverse Agonists ◽  
Pharmacological Evaluation

Effects of cannabinoids on endogenous K+ and Ca2+ currents in HEK293 cells

2003 ◽  
Vol 81 (5) ◽  
pp. 436-442 ◽  
Author(s):  
Clemente Vásquez ◽  
Ricardo A Navarro-Polanco ◽  
Miguel Huerta ◽  
Xóchitl Trujillo ◽  
Felipa Andrade ◽  
...  
Keyword(s):  
Cannabinoid Receptor ◽  
Inward Rectifier ◽  
Calcium Currents ◽  
Hek293 Cells ◽  
Delayed Rectifier ◽  
Patch Clamp Technique ◽  
Inverse Agonists ◽  
Cb1 Cannabinoid Receptor ◽  
Cell Variant ◽  
Cannabinoid Agonists

Effects of cannabinoids on endogenous potassium and calcium currents in HEK293 cells were studied using the whole-cell variant of the patch-clamp technique. The cannabinoid agonists WIN 55,212-2, methanandamide, and anandamide (1 μM) decreased the calcium current by 53.1 ± 2.6, 47.5 ± 1.2, and 38.8 ± 3.1%, respectively, after transfection of human CB1 cannabinoid receptor (hCB1) cDNA into HEK293 cells. The delayed rectifier-like current was not changed after application of these agonists, but the inward rectifier was increased by 94.0 ± 3.6, 83.7 ± 5.1, and 63.0 ± 2.5% after application of WIN 55,212-2, methanandamide, and anandamide, respectively. The effects of the cannabinoid antagonists (AM251, AM281, and AM630) on the inward rectifier and calcium currents were the opposite of those seen with cannabinoid agonists; thus, these compounds act as inverse agonists in this preparation. These results suggest that endogenous inward rectifier and calcium currents are modulated by cannabinoids in HEK293 cells, and that some expressed receptors may be constitutively active.Key words: cannabinoids, WIN 55,212-2, anandamide, methanandamide, inverse agonists.

Bioisosteric replacement of the pyrazole 3-carboxamide moiety of rimonabant. A novel series of oxadiazoles as CB1 cannabinoid receptor antagonists

2008 ◽  
Vol 6 (18) ◽  
pp. 3399 ◽  
Author(s):  
Cheng-Ming Chu ◽  
Ming-Shiu Hung ◽  
Min-Tsang Hsieh ◽  
Chun-Wei Kuo ◽  
Suja T. D. ◽  
...  
Keyword(s):  
Cannabinoid Receptor ◽  
Receptor Antagonists ◽  
Bioisosteric Replacement ◽  
Cb1 Cannabinoid Receptor

Falcarinol (Panaxynol) is a CB1 cannabinoid receptor antagonist and induces pro-allergic effects in skin

Planta Medica ◽  
2009 ◽  
Vol 75 (09) ◽  
Author(s):  
J Gertsch ◽  
M Leonti ◽  
L Casu ◽  
F Cottiglia ◽  
S Raduner ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Cannabinoid Receptor ◽  
Cb1 Cannabinoid Receptor
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