Evaluation of a series of N-alkyl benzomorphans in cell lines expressing transfected delta- and mu-opioid receptors

Biochemical Pharmacology
M E AboodL S Harris

Abstract

Transfection of individual opioid receptors in Chinese hamster ovary (CHO) cells provides a pure, homogeneous population of receptors for screening drug candidates, and an alternative to the use of selective ligands. To evaluate the potential of this system, we chose a series of (-)-5,9 alpha-dimethyl-2-hydroxy-N-substituted-6,7-benzomorphans, for which the receptor selectivity and in vivo activity had been characterized recently, and tested them in CHO cells stably transfected with either the rat delta-opioid receptor or the mouse mu-opioid receptor. [3H]Diprenorphine was used to measure opioid receptors in P2 membrane preparations. A Bmax of 7.58 +/- 0.8 pmol/mg protein and a Kd of 0.42 +/- 0.04 nM was obtained in the mu-opioid receptor expressing cell line used in these studies. In addition, [3H]naltrindole was used to confirm the delta-specificity of the cloned receptor. Both compounds gave a Bmax of 1.2 pmol/mg in the CHO cells expressing the rat delta-opioid receptor. Displacement assays were performed with eleven (-)-N-alkyl-benzomorphans in the absence and presence of 150 mM NaCl, as well as known delta- and mu-selective agonists. Sodium reduced agonist affinity in the transfected cell lines. The benzomorphan compounds ...Continue Reading

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