Mixed inhibitors of aminopeptidase N and neprilysin are disclosed. Pharmaceutical compositions containing at least one of these compounds, used alone or in combination with morphine and derivatives thereof, endocannabinoids and inhibitors of endocannabinoid metabolism, GABA derivatives such as gabapentin or pregabalin, duloxetine or methadone, can be used as an analgesic, anxiolytic, antidepressant or anti-inflammatory.胺肽酶N與腦啡肽酶之混合抑制劑係揭露的。藥學組成物其含有這些化合物中至少一者,單獨或與嗎啡及其衍生物、內源性大麻素及內源性大麻素代謝的抑制劑、諸如佳巴本汀(gabapentin)或普瑞巴林(pregabalin)之GABA衍生物、杜洛希酊(duloxetine)或美沙酮組合使用的,可以使用作為鎮痛劑、抗焦慮劑、抗抑鬱劑或抗發炎。