PROBLEM TO BE SOLVED: To provide methods of enhancing normal melanocortin-4 receptor (MC4R) activity, and a method of treating an individual having a condition in which increased activity of an MC4R at the cell surface is beneficial, for example in obesity, by administering an effective amount of a pharmacological chaperone for the MC4R.SOLUTION: The pharmacological chaperone is an MC4R antagonist represented by figure 1. A pharmacological chaperone for MC4R is a molecule that binds to MC4R, resulting in proper folding, trafficking, non-aggregation, and activity of MC4R. The method comprises administering an effective amount of the pharmacological chaperone.SELECTED DRAWING: Figure 1【課題】正常なメラノコルチン4受容体(MC4R)活性を促進する方法、及び、細胞表面のMC4Rの活性増加が有益である状態(例えば、肥満のような)である個体を、MC4Rに対して有効な量の薬理学的シャペロンの投与によって治療する方法の提供。【解決手段】薬理学的シャペロンは図1で例示されるMC4Rアンタゴニストであり、MC4Rに対する薬理学的シャペロンは、MC4Rの適切な折畳み、輸送、非凝集及び活性をもたらす、MC4Rと結合する分子であり、その有効量を投与する方法。【選択図】図1