Weissman A D, Casanova M F, Kleinman J E, London E D, De Souza E B
Neuroscience Branch, National Institute on Drug Abuse, Baltimore, MD 21224.
Biol Psychiatry. 1991 Jan 1;29(1):41-54. doi: 10.1016/0006-3223(91)90209-5.
Drugs such as phencyclidine (PCP) that interact with PCP and sigma binding sites can produce psychotomimetic effects that resemble some symptoms of schizophrenia. Therefore, it has been suggested that PCP and sigma receptors may be important in the clinical manifestations of schizophrenia. Assays of these two binding sites in human postmortem brains showed consistent significant reductions in the density of sigma, but not PCP sites, in schizophrenics as compared with age-matched and postmortem interval-matched normal and suicide controls. Reductions in the density of sigma binding sites in schizophrenia were most prominent in temporal cerebral cortex, and were accompanied by a small increase in affinity for the ligand [3H]haloperidol. These data provide the first evidence for alterations in sigma binding sites in schizophrenia, and suggest that selective sigma ligands may be useful in the treatment of the disorder.
诸如苯环己哌啶（PCP）这类与PCP及西格玛结合位点相互作用的药物，可产生类似精神分裂症某些症状的拟精神病效应。因此，有人提出PCP和西格玛受体可能在精神分裂症的临床表现中起重要作用。对人类死后大脑中这两个结合位点的检测显示，与年龄匹配、死后间隔时间匹配的正常人和自杀对照组相比，精神分裂症患者的西格玛结合位点密度持续显著降低，但PCP结合位点密度并未降低。精神分裂症患者中，西格玛结合位点密度的降低在颞叶大脑皮质最为显著，并且伴随着对配体[3H]氟哌啶醇亲和力的小幅增加。这些数据首次证明了精神分裂症中西格玛结合位点的改变，并表明选择性西格玛配体可能对治疗该疾病有用。
