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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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 740-746 (November 2000) DOI: 10.1093/bja/85.5.740 Copyright © 2000 British Journal of Anaesthesia Terms and Conditions

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 2000 85, 740-746DOI: (10.1093/bja/85.5.740) Copyright © 2000 British Journal of Anaesthesia Terms and Conditions

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 2000 85, 740-746DOI: (10.1093/bja/85.5.740) Copyright © 2000 British Journal of Anaesthesia Terms and Conditions

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 2000 85, 740-746DOI: (10.1093/bja/85.5.740) Copyright © 2000 British Journal of Anaesthesia Terms and Conditions