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Description of a Bivalent Cannabinoid Ligand with Hypophagic Properties
Author(s) -
FernándezFernández Cristina,
Decara Juan,
BermúdezSilva Francisco J.,
Sánchez Eva,
Morales Paula,
GómezCañas María,
GómezRuíz María,
Callado Luis F.,
Goya Pilar,
Rodríguez de Fonseca Fernando,
Martín M. Isabel,
FernándezRuíz Javier,
Meana J. Javier,
Jagerovic Nadine
Publication year - 2013
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201200392
Subject(s) - cannabinoid receptor , cannabinoid , rimonabant , bivalent (engine) , chemistry , in vivo , pharmacology , receptor , stereochemistry , cannabinoid receptor type 2 , biochemistry , antagonist , biology , organic chemistry , microbiology and biotechnology , metal
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.