Opioid agonists binding data

Fig. 37.4. Spectral map of the 26 opioid agonists and antagonists in 4 receptor binding tests, as described by Table 37.7 [45, 46]. Circles refer to the compounds. Squares represent the binding tests. Areas of circles and squares are proportional to the marginal mean affinities in the table. The lines that join the three poles (DHM, DADLE and EKC) of the map represent axes of contrast between the p-, 8-and K-opioid receptors. The horizontal and vertical components represent 18 and 79%, respectively, of the interaction in the data.

To develop highly potent, selective, and efficacious delta agonists of potential therapeutic value, the Molecular Pharmacology Department at AstraZeneca R D Montreal has established and implemented binding and functional assays for all three human opioid receptors [11]. These assays were used to provide in vitro pharmacological data to support the design, synthesis, and analysis of newer generations of delta selective compounds. In the... 

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