Chimerization of tachykinin and opioid pharmacophores offers a new avenue for analgesic development. The complexities of such design are illustrated by the analgesic efficacy (via different mechanisms) of chimeras that combine pharmacophores with opioid activity and substance P activity, as well as those that combine opioid agonist and substance P antagonist moieties. Although the interaction between substance P and opioid neural systems is more complex than a simple one-way inhibition, the relative balance of activities between tachykinin and opioid pharmacophores will generally determine the net effect of the chimeric molecule as pro-nociceptive, antinociceptive, or neutral. Intriguingly, endomorphins - mu opioid receptor agonists with high intrinsic activity - may owe some of this high activity to weak but significant antagonist properties at tachykinin receptors, implying that these native peptides are endogenous chimeric opioid agonist + tachykinin antagonist compounds. The modification of basic endomorphin I sequence resulted in analogues with increased affinities to tachykinin, especially NK1 receptors.

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