Koe B K, Burkhart C A, Lebel L A
Department of Pharmacology, Central Research Division, Pfizer Inc., Groton, CT 06340.
Eur J Pharmacol. 1989 Feb 28;161(2-3):263-6. doi: 10.1016/0014-2999(89)90857-1.
Binding of i.v. administered (+)-[3H]3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ([3H]3-PPP) in the brain of intact mice is antagonized dose responsively by sigma receptor ligands. The correlation of potencies for inhibition of binding in vivo and in vitro indicates that sigma receptors in mouse brain are labeled in vivo by i.v. [3H]3-PPP. 3-PPPP, the N-phenylpropyl derivative of norpropyl-3-PPP exhibits very high affinity for sigma receptors in vitro and in vivo.
静脉注射给予的（+）-[3H]3-（3-羟基苯基）-N-（1-丙基）哌啶（[3H]3-PPP）在完整小鼠脑中的结合被σ受体配体以剂量反应方式拮抗。体内和体外结合抑制效力的相关性表明，小鼠脑中的σ受体在体内被静脉注射的[3H]3-PPP标记。3-PPPP，即去丙基-3-PPP的N-苯基丙基衍生物，在体外和体内对σ受体均表现出非常高的亲和力。
