Modell S, Naber D, Holzbach R
Department of Psychiatry, University of Munich, Germany.
Pharmacopsychiatry. 1996 Mar;29(2):63-6. doi: 10.1055/s-2007-979546.
The psychotomimetic effects of opiate agonists/antagonists led to the hypothesis that opiate sigma receptors could be involved in the etiology of schizophrenia. This assumption is supported by animal trials with selective sigma-receptor antagonists. SL 82.0715 is a substance with a highly selective affinity for sigma receptors. To clarify the question whether it improves negative symptoms of schizophrenia, ten chronic schizophrenic patients with a predominant negative symptomatology were examined and treated with increasing doses (2.5 - 10.0 mg/d). Psychopathology was evaluated weekly using the PANSS, BPRS, and CGI, side-effects were assessed by the HAS and the S/A scale. Four patients showed improvement of negative symptoms (two slight, two marked improvement), two patients deteriorated as regards the positive symptomatology, psychopathology in the other patients did not change. The tolerability of SL 82.0715 was very good, no extrapyramidal side-effects occurred. To further evaluate the therapeutic efficacy, open studies with a larger number of patients and/or double-blind studies are necessary.
阿片类激动剂/拮抗剂的拟精神病效应引发了这样一种假说，即阿片类西格玛受体可能参与了精神分裂症的病因学。这一假设得到了使用选择性西格玛受体拮抗剂的动物试验的支持。SL 82.0715是一种对西格玛受体具有高度选择性亲和力的物质。为了阐明它是否能改善精神分裂症的阴性症状，对10名以阴性症状为主的慢性精神分裂症患者进行了检查，并给予递增剂量（2.5 - 10.0毫克/天）的治疗。每周使用阳性和阴性症状量表（PANSS）、简明精神病评定量表（BPRS）和临床总体印象量表（CGI）评估精神病理学，通过不良反应量表（HAS）和症状/不良反应量表（S/A）评估副作用。4名患者的阴性症状有所改善（2名略有改善，2名明显改善），2名患者的阳性症状恶化，其他患者的精神病理学没有变化。SL 82.0715的耐受性非常好，未出现锥体外系副作用。为了进一步评估治疗效果，有必要对更多患者进行开放性研究和/或双盲研究。
