Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 14, Issue 2, Pages 491-493Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2003.10.048
Keywords
I-2-imidazoline binding site affinity; mu-opioid affinity; alane guanidine; dual acting drug; opioid tolerance; opioid withdrawal; human brain
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A 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 V opioid receptors and for the I-2-imidazoline binding sites (I-2-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. (C) 2003 Elsevier Ltd. All rights reserved.
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