SKF 525A, a classical inhibitor of microsomal drug-metabolizing enzymes, is structurally similar to the diphenylpropylamine analgesics, and certain reported effects in animals resemble those produced by opiate drugs. In an opiate radioreceptor assay, SKF 525A was 50 times less potent than methadone in the absence of sodium and 10 times less potent in the presence of sodium. The nature of the sodium effect indicates SKF 525A to have less opiate agonist character than does methadone. In mice, 2 mg of SKF 525A given intraperitoneally induced less profound analgesia on a hot plate (44 °C) than did 0.1 mg of methadone. Analgesia by SKF 525A was prevented by pretreatment of the mice with naloxone. In rats, 50 μg of SKF 525A given intracerebroventricularly was analgesic.