Invention of superagonists and superantagonists for ORL1 nociceptin receptor

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The principal objective of this project is to carry out so-called total Ala-scanning of ORL1 nociceptin receptor and then to identify the residues essential for the receptor activation. To date, the Ala-scanning was achieved with successful Ala-mutation of more than 247 scheduled-residues (270 in total), and further the more than 10 of amino acid residues were explored as essentials for the receptor activation. Eventually, we achieved the establishment in general molecular design of ligands that work for activity enhancement or suppression by bind or interfere specifically for these residues.