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Type: Journal article
Title: Naloxone and its quaternary derivative, naloxone methiodide, have differing affinities for m, d, k and opiod receptors in mouse brain homogenates
Author: Lewanowitsch, T.
Irvine, R.
Citation: Brain Research, 2003; 964(2):302-305
Publisher: Elsevier Science Bv
Issue Date: 2003
ISSN: 0006-8993
Statement of
Tanya Lewanowitsch and Rodney James Irvine
Abstract: Naloxone and naloxone methiodide both act on opioid receptors but naloxone methiodide has limited access to the brain. Naloxone methiodide has been shown to have a lower affinity for opioid receptors than naloxone in the rat and guinea pig but has not been tested in the mouse. We aimed to investigate this by using [3H]DAMGO, [3H]DPDPE and [3H]U-69,593 to compare the ability of naloxone and naloxone methiodide to displace binding to μ, δ and κ opioid receptors in mouse brain homogenates. Significant binding was observed for each receptor type and the binding affinity for naloxone versus naloxone methiodide was found to be 15:1 for μ, 6:1 for κ and 330:1 for δ receptors. Therefore, naloxone methiodide does have a lower affinity for opioid receptors than naloxone in mouse brain tissue, which must be taken into consideration in experimental designs.
Keywords: Naloxone
Naloxone methiodide
Opioid receptor
Description: Copyright © 2002 Elsevier Science B.V. All rights reserved.
DOI: 10.1016/S0006-8993(02)04117-3
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Pharmacology publications

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