Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/44349
Título : CB1 cannabinoid antagonists: Structure-activity relationships and potential therapeutic applications
Autor : Jagerovic, Nadine, Fernandez-Fernandez, Cristina, Goya, Pilar
Palabras clave : Cannabinoid
antagonist
CB1
rimonabant
endocannabinoid
Fecha de publicación : Feb-2008
Editor: Bentham Science Publishers
Citación : Current Topics in Medicinal Chemistry 8 (3) : 205-230 (2008)
Resumen: During the last decade there has been a growing interest towards the modulation of the cannabinoid CB1 receptor. The identification of CB1 cannabinoid receptor antagonists has been one of the major advances in cannabinoid research. Thus, the development of these ligands has opened new therapeutic applications. Since the discovery of the first cannabinoid receptor antagonist, rimonabant, by Sanofi in 1994, a large number of structural variations within this chemical series of 1,5-diarylpyrazoles have been described. So far, all attempts to identify novel structures for CB1 antagonists have been based on one or more pharmacophoric elements of the rimonabant structure. The advanced clinical trials of rimonabant confirm the therapeutic potential value of CB1 antagonists for the treatment of obesity. In addition, the results of pharmacological and clinical studies reveal other effective pharmacotherapeutic applications. The current review will mainly focus on the structure-activity relationships that have been established for antagonists/inverse agonists that bind to the CB1 cannabinoid receptors and on their therapeutic applications
Versión del editor: http://dx.doi.org/10.2174/156802608783498050
URI : http://hdl.handle.net/10261/44349
ISSN: 1568-0266
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