Disclosed is an in vitro screening method for identifying an antagonist-to-agonist allosteric modifier of a mu-opioid receptor and an in vivo method for confirming that a test compound is such a modifier of a mu-opioid receptor. Also disclosed is a method for treating an opioid receptor-associated condition using a compound of Formula (I) and a pharmaceutical composition containing the same.本揭露係關於一種用以檢測一μ鴉片受體拮抗劑轉促效劑之異構調節劑的體外篩選方法,以及一種確認受試化合物為一μ鴉片受體之調節劑的體內確認方法。本揭露更提供一種使用如式(I)所示之化合物用以治療鴉片受體相關病症之方法及包含此化合物之醫藥組成物。