| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject antagonist simultaneously showing affinity for ORL1 receptor and antagonism against nociceptin by including a specific compound as an active ingredient. SOLUTION: This antagonist comprises a compound of formula I [a double wavy line is a double bond or a single bond; R1 is a 1-5C alkyl, a 4-7C cycloalkyl, a 7-13C aralkyl or the like; R2 and R3 are each H, hydroxyl, a 1-5C alkanoyloxy or the like; A is XC(=Y) (X is S, O or the like; Y is O), X or the like; R4 is H or a 1-5C alkyl; B is a valence bond, a 1-14C alkylene, a 2-14C noncyclic unsaturated hydrocarbon or the like; R5 is H or an organic group containing a basic skeleton of formula II or the like; R6 is H; R7 is H, hydroxyl, a 1-5C alkyl or the like; R8 is H or a 1-5C alkyl] as an active ingredient. In the case of injection for example, the amount of the active ingredient is about 0.0001 mg to 1 g daily.
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