Abstract

The effects of 2'-hydroxy-5,9-dimethyl-2-(3,3-dimethylallyl)-6,7-benzomorphan (Win 20,228) a weak narcotic antagonist, have been studied in man. In the treatment of postoperative pain 10-20 mg/70 kg of Win 20,228 produced analgesia equivalent to 10 mg/70 kg of morphine. The degree of respiratory depression produced by 20 mg/70 kg of Win 20,228 was comparable to that of 10 mg/70 kg of morphine. The subjective effects of Win 20,228 were qualitatively and quantitatively similar to those of morphine. Except for one patient who reported "crazy thoughts," nalorphine-like psychotomimetic effects were not observed in other patients or healthy subjects.

Win 20,228 was shown to be a weak antagonist of morphine induced respiratory depression and the respiratory depression of Win 20,228 was not antagonized by potent narcotic antagonists. In contrast to morphine, Win 20,228 in doses greater than 2 mg/kg intravenously produced tachycardia and hypertension. Win 20,228 may represent the first clinically useful potent analgesic with minimal addiction liability.