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Fentanyl derivatives bearing aliphatic alkaneguanidinium moieties: A new series of hybrid molecules with significant binding affinity for μ-opioid receptors and I2-imidazoline binding sites

AuthorsDardonville, Christophe ; Jagerovic, Nadine ; Callado, Luis F.; Meana, J. J.
Issue Date2004
PublisherPergamon Press
CitationBioorganic and Medicinal Chemistry Letters 14: 491- 493 (2004)
AbstractA new series of fentanyl derivatives [i.e., N-[1-(2-phenethyl)-4-piperidyl] -N-(guanidinoalkyl)propanamide] bearing aliphatic alkaneguanidinium moieties were prepared. Their affinities for the μ opioid receptors and for the I 2-imidazoline binding sites (I2-IBS) were determined on human post-mortem prefrontal cortex membranes. All of these hybrid compounds had significant and/or very high affinity for both receptors in the nanomolar range, meaning an improvement compared to the prototype N-[1-(2-phenethyl)-4- piperidyl]-N-(guanidinopropyl)propanamide previously reported. © 2003 Elsevier Ltd. All rights reserved.
Identifiersdoi: 10.1016/j.bmcl.2003.10.048
issn: 0960-894X
e-issn: 1464-3405
Appears in Collections:(IQM) Artículos
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