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Most often, a compromise has to be made between these mutually opposing characteristics.<\/jats:p><jats:p>In this study, Derringer's desirability function, a multi\u2010criteria decision\u2010making method, was applied to determine the best peptide for opioid studies in a single figure\u2010of\u2010merit.<\/jats:p><jats:p>The penetration of the blood\u2013brain barrier (BBB) determines the biological functionality of neuropeptides in the brain target tissue, and consists of an influx and an efflux component. The metabolic stability in the two concerned tissues, i.e. plasma and brain, are taken into consideration as well. The overall selection of the peptide drug candidate having the highest BBB\u2010drugability is difficult due to these conflicting responses as well as the different scalings of the four biological parameters under consideration.<\/jats:p><jats:p>The highest desirability, representing the best BBB\u2010drugability, was observed for dermorphin. This peptide is thus the most promising drug candidate from the set of eight opioid peptides that were investigated. The least desirable candidate, with the worst BBB influx and\/or metabolic stability, was found to be CTAP. Validation of the desirability function by<jats:italic>in vivo<\/jats:italic>medical imaging showed that dermorphin and DAMGO penetrate the BBB, whereas EM\u20101 and TAPP did not. These results are thus consistent with those obtained with the desirability evaluation.<\/jats:p><jats:p>To conclude, the multi\u2010criteria decision method was proven to be useful in biomedical research, where a selection of the best candidate based on opposing characteristics is often required. 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