Steinfels G F, Tam S W
E.I. du Pont de Nemours & Co., Inc., Medical Products Department, Wilmington, DE 19880-0400.
Eur J Pharmacol. 1989 Apr 12;163(1):167-70. doi: 10.1016/0014-2999(89)90413-5.
Extracellular recording techniques were used to study the effects of the selective sigma receptor agonist (+)-[3H]3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ((+)-3-PPP) and selective sigma receptor antagonist BMY 14802 on dopamine (DA) neurons of the substantia nigra. Intravenous administration of (+)-3-PPP produced a dose-dependent inhibition of DA neuron firing rate. Complete inhibition of DA neurons produced by (+)-3-PPP could be completely reversed by administration of BMY 14802. Also, pretreatment with BMY 14802 shifted the (+)-3-PPP dose response curve to the right. These data demonstrate a relationship of the sigma receptor with the dopamine system and further suggest a model system to study agonist/antagonist interactions of sigma ligands.
采用细胞外记录技术研究选择性σ受体激动剂（+）-[3H]3-（3-羟基苯基）-N-（1-丙基）哌啶（（+）-3-PPP）和选择性σ受体拮抗剂BMY 14802对黑质多巴胺（DA）神经元的影响。静脉注射（+）-3-PPP可产生剂量依赖性抑制DA神经元放电率。（+）-3-PPP对DA神经元的完全抑制可通过给予BMY 14802完全逆转。此外，用BMY 14802预处理可使（+）-3-PPP剂量反应曲线右移。这些数据证明了σ受体与多巴胺系统之间的关系，并进一步提示了一个研究σ配体激动剂/拮抗剂相互作用的模型系统。
