Su T P, Schell S E, Ford-Rice F Y, London E D
Neuropharmacology Laboratory, National Institute on Drug Abuse, Baltimore, Maryland 21224.
Eur J Pharmacol. 1988 Apr 13;148(3):467-70. doi: 10.1016/0014-2999(88)90130-6.
The putative sigma receptor antagonists, haloperidol, HR 375, BMY 14802 and BW 234U potently inhibited both [3H]d-N-allylnormetazocine binding to sigma receptors in brain homogenates and [3H]haloperidol binding to sigma receptors in spleen homogenates. An excellent correlation of inhibitory potencies in the two assay systems was obtained. The results support the view that [3H]d-N-allylnormetazocine and [3H]haloperidol both label the same receptor populations, and suggest that sigma antagonists may be useful in elucidating physiological role(s) of sigma receptors in the nervous and immune systems.
假定的σ受体拮抗剂氟哌啶醇、HR 375、BMY 14802和BW 234U均能有效抑制[3H]d-N-烯丙基去甲左啡诺与脑匀浆中σ受体的结合以及[3H]氟哌啶醇与脾匀浆中σ受体的结合。在这两种检测系统中获得了抑制效力的良好相关性。结果支持[3H]d-N-烯丙基去甲左啡诺和[3H]氟哌啶醇均标记相同受体群体的观点，并表明σ受体拮抗剂可能有助于阐明σ受体在神经和免疫系统中的生理作用。
