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Title

Description of a bivalent cannabinoid ligand with hypophagic properties

AuthorsFernández-Fernández, Cristina ; Decara, Juan; Bermúdez-Silva, Francisco Javier; Sánchez, Eva; Morales, Paula ; Gõmez-Cañas, María; Gõmez-Ruíz, María; Callado, Luis F.; Goya, Pilar ; Rodríguez De Fonseca, Fernando; Martín, M. Isabel ; Fernández-Ruiz, Javier; Meana, J. Javier; Jagerovic, Nadine
KeywordsBivalent ligand
Cannabinoid receptors
CB1
Food intake
Rimonabant
Issue Date2013
PublisherJohn Wiley & Sons
CitationArchiv der Pharmazie 346: 171- 179 (2013)
AbstractA series of bivalent cannabinoid ligands is proposed. The synthesis of double amides based on the rimonabant structure separated by an alkyl chain and the evaluation of their affinities for cannabinoid receptors are reported. The data of 4d confirmed that a bivalent structure is a suitable scaffold for CB1 cannabinoid receptor binding. The compound 4d was selected for in vitro and in vivo pharmacological evaluations. Moreover, intraperitoneal administration of 4d to food-deprived rats resulted in a dose-dependent inhibition of feeding that was maintained up to 240 min. A series of bivalent cannabinoid ligands was synthesized. The data of 4d confirmed that a bivalent structure is a suitable scaffold for CB1 cannabinoid receptor binding. The compound 4d was selected for in vitro and in vivo pharmacological evaluations. Moreover, intraperitoneal administration of 4d to food-deprived rats resulted in a dose-dependent inhibition of feeding that was maintained up to 240 min. © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
URIhttp://hdl.handle.net/10261/99683
DOI10.1002/ardp.201200392
Identifiersdoi: 10.1002/ardp.201200392
issn: 0365-6233
e-issn: 1521-4184
Appears in Collections:(IQM) Artículos
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