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Interaction of local anaesthetics with recombinant μ, κ, and δ-opioid receptors expressed in Chinese hamster ovary cells  K. Hirota, H. Okawa, B.L. Appadu,

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Presentation on theme: "Interaction of local anaesthetics with recombinant μ, κ, and δ-opioid receptors expressed in Chinese hamster ovary cells  K. Hirota, H. Okawa, B.L. Appadu,"— Presentation transcript:

1 Interaction of local anaesthetics with recombinant μ, κ, and δ-opioid receptors expressed in Chinese hamster ovary cells  K. Hirota, H. Okawa, B.L. Appadu, D.K. Grandy, D.G. Lambert  British Journal of Anaesthesia  Volume 85, Issue 5, Pages (November 2000) DOI: /bja/ Copyright © 2000 British Journal of Anaesthesia Terms and Conditions

2 Fig 1 (a) Lidocaine concentration-dependently displaced [3H]DPN from CHO-κ, μ and δ with the following rank order: κ > μ > δ. (b) Interaction of a range of local anaesthetics with μ-opioid receptor. Concentration– response curves are corrected for the competing mass of [3H]DPN according to Cheng and Prusoff.23 All data are mean (SEM) (n=5). British Journal of Anaesthesia  , DOI: ( /bja/ ) Copyright © 2000 British Journal of Anaesthesia Terms and Conditions

3 Fig 2 Interaction of bupivacaine isomers with μ- (a), κ- (b) and δ (c)-opioid receptors. All data are mean (sem) (n=5). For CHO-μ and -κ, there is a suggestion of stereoselectivity (i.e. the curve for S(–)bupivacaine tends to the right). British Journal of Anaesthesia  , DOI: ( /bja/ ) Copyright © 2000 British Journal of Anaesthesia Terms and Conditions

4 Fig 3 (a) Lidocaine produced a concentration-dependent inhibition of forskolin-stimulated cAMP formation in CHO cells expressing μ, κ, δ opioid receptors (CHO-μ, κ, δ) and in untransfected wt cells. (b) Lidocaine-induced inhibition of forskolin-stimulated cAMP formation was naloxone insensitive. All data are mean (SEM) (n=4–5). British Journal of Anaesthesia  , DOI: ( /bja/ ) Copyright © 2000 British Journal of Anaesthesia Terms and Conditions


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