Synthesis and pharmacological studies of new hybrid derivatives of fentanyl active at the μ-opioid receptor and I 2–imidazoline binding sites

…, C Fernandez-Fernandez, SL Gibbons, GJ Ryan…

Index: Dardonville, Christophe; Fernandez-Fernandez, Cristina; Gibbons, Sarah-Louise; Ryan, Gary J.; Jagerovic, Nadine; Gabilondo, Ane M.; Meana, J. Javier; Callado, Luis F. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 19 p. 6570 - 6580

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Citation Number: 53

Abstract

Two series of fentanyl-derived hybrid molecules bearing potent I2–imidazoline binding site (IBS) ligands (ie, guanidine and BU224 moieties) linked with an aliphatic (m= 2, 3, 4, 6, 7, 8, 9 and 12 methylene units) or aromatic spacer were prepared. Their affinities for the μ-opioid receptors and for the I2–IBS were determined through competition binding studies on human postmortem brain membranes. Whereas the BU224 hybrid molecules bound to the ...