Ho T K, LaBella F S, Pinsky C
Can J Physiol Pharmacol. 1978 Aug;56(4):550-4. doi: 10.1139/y78-088.
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 prescence 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 degrees C) than did 0.1 mg of methadone. Analgesia by SKF 525A was prevented by pretreatment of the mice with naloxone. In rats, 50 microgram of SKF 525A given intracerebroventricularly was analgesic.
SKF 525A是一种经典的微粒体药物代谢酶抑制剂，其结构与二苯基丙胺类镇痛药相似，并且某些在动物身上报道的效应类似于阿片类药物产生的效应。在阿片类放射受体测定中，在无钠情况下SKF 525A的效力比美沙酮低50倍，在有钠存在时效力比美沙酮低10倍。钠效应的性质表明SKF 525A的阿片激动剂特性比美沙酮少。在小鼠中，腹腔注射2毫克SKF 525A在热板（44摄氏度）上引起的镇痛作用不如0.1毫克美沙酮深刻。用纳洛酮预处理小鼠可防止SKF 525A产生镇痛作用。在大鼠中，脑室内注射50微克SKF 525A具有镇痛作用。
