Abstract: The present invention provides a compound having a selective opioid ? receptor agonist effect. The present invention provides a pyrazolomorphinan derivative represented by general formula (1) (in the formula, (II) R1 represents a hydrogen atom, an alkyl group, a cycloalkylmethyl group, or the like, R2 represents a hydrogen atom or a hydroxy protecting group, R3 represents a hydroxy group, an alkyl group, a partially unsaturated heterocyclic group, an aryl group, a heteroaryl group, or the like; and R4 represents a hydrogen atom, an alkyl group, an aralkyl group, a cycloalkyl group, a cycloalkyl alkyl group, a saturated heterocyclic group, an aryl group, a heteroaryl group, or the like). The pyrazolomorphinan derivative can be used as an active ingredient in an analgesic, an antidepressant, an anxiolytic, or the like.