Description of a Bivalent Cannabinoid Ligand with Hypophagic Properties
,
Marı́a Gómez-Cañas ,
M. Isabel Martín,
Pilar Goya,
M. Isabel Martín,
Javier Fernández-Ruíz,
Fernando Rodríguez de Fonseca,
J. Javier Meana
and other authors.
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Abstract
A 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 CB(1) 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.