• Brain research · Feb 2003

    Naloxone and its quaternary derivative, naloxone methiodide, have differing affinities for mu, delta, and kappa opioid receptors in mouse brain homogenates.

    • Tanya Lewanowitsch and Rodney James Irvine.
    • Department of Clinical and Experimental Pharmacology, 5th Floor, Medical School North, University of Adelaide, South Australia 5005, Adelaide, Australia. tanya.lewanowitsch@adelaid.edu.au
    • Brain Res. 2003 Feb 28; 964 (2): 302-5.

    AbstractNaloxone 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 mu, delta and kappa 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 mu, 6:1 for kappa and 330:1 for delta 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.

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