Verhoeven W M, van Ree J M, Heezius-van Bentum A, de Wied D, van Praag H M
Arch Gen Psychiatry. 1982 Jun;39(6):648-54. doi: 10.1001/archpsyc.1982.04290060010003.
Animal experiments have shown that the gamma-endorphin fragment des-enkephalin-gamma-endorphin (DE gamma E; beta-lipotropin 66-77) is the shortest sequence with neuroleptic-like activity with potency comparable to des-tyrosine-gamma-endorphin. We postulated that DE gamma E may be an endogenous peptide implicated in psychopathologic disease, particularly schizophrenia. To investigate the purported antipsychotic action of DE gamma E, 23 patients with different types of relapsing schizophrenia were treated with DE gamma E dissolved in saline or placebo. Neuroleptic medication was continued during the experimental period. In the first single-blind trial, two patients were treated with 1 mg of DE gamma E and two with 10 mg of DE gamma E intramuscularly (IM) daily for ten days. In the second double-blind placebo-controlled trial 13 patients were treated with 3 mg of DE gamma E IM daily for ten days and six received placebo. Of the 17 patients treated with DE gamma E, two did not respond, 11 had a slight to moderate effect, and four responded markedly. No side effects were observed. The response to DE gamma E appeared to be negatively correlated with the dosage of neuroleptic medication and the duration of the last psychotic episode. These results support the hypothesis that disturbances in gamma-endorphin fragmentation might contribute to the pathogenesis of schizophrenic psychoses.
动物实验表明，γ-内啡肽片段脱脑啡肽-γ-内啡肽（DEγE；β-促脂素66-77）是具有抗精神病样活性的最短序列，其效力与脱酪氨酸-γ-内啡肽相当。我们推测DEγE可能是一种与精神病理疾病，尤其是精神分裂症有关的内源性肽。为了研究DEγE所谓的抗精神病作用，23例不同类型的复发性精神分裂症患者接受了溶解于生理盐水的DEγE或安慰剂治疗。在实验期间继续使用抗精神病药物。在第一个单盲试验中，两名患者每天肌肉注射（IM）1毫克DEγE，两名患者每天肌肉注射10毫克DEγE，持续十天。在第二个双盲安慰剂对照试验中，13例患者每天肌肉注射3毫克DEγE，持续十天，6例接受安慰剂。在接受DEγE治疗的17例患者中，2例无反应，11例有轻微至中度疗效，4例有明显反应。未观察到副作用。对DEγE的反应似乎与抗精神病药物的剂量和最后一次精神病发作的持续时间呈负相关。这些结果支持了γ-内啡肽片段化紊乱可能导致精神分裂症性精神病发病机制的假说。
