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（+）-3-苯基-1-哌嗪丙腈拮抗（+）-N-烯丙基去甲左啡诺的辨别刺激效应。

(+)-3-PPP antagonizes the discriminative stimulus effects of (+)-N-allylnormetazocine.

作者信息

Balster R L

出版信息

Eur J Pharmacol. 1986 Aug 15;127(3):283-6. doi: 10.1016/0014-2999(86)90377-8.

DOI:10.1016/0014-2999(86)90377-8
PMID:3019734
Abstract

The functional significance of the reported affinity of (+)-3-PPP and (+)-N-allylnormetazocine (NANM) for the same binding site in rat brain membranes was assessed by studying (+)-3-PPP as a agonist and antagonist of (+)-NANM in rats trained to discriminate 5.0 mg/kg (+)-NANM from saline. Over a wide dose range, (+)-3-PPP was able to block the discriminative stimulus effects of (+)-NANM, with complete antagonism at 1.0 mg/kg i.p. Since (+)-NANM is a prototype sigma-opioid agonist, (+)-3-PPP is a good candidate for being a competitive sigma antagonist.

摘要

通过在经过训练可区分5.0毫克/千克（+）-烯丙基去甲佐辛（NANM）和生理盐水的大鼠中，研究（+）-3-苯基-1-丙基哌嗪（+）-3-PPP）作为（+）-NANM的激动剂和拮抗剂，评估了所报道的（+）-3-PPP和（+）-烯丙基去甲佐辛（NANM）对大鼠脑膜中同一结合位点的亲和力的功能意义。在很宽的剂量范围内，（+）-3-PPP能够阻断（+）-NANM的辨别刺激效应，腹腔注射1.0毫克/千克时完全拮抗。由于（+）-NANM是一种典型的σ-阿片受体激动剂，（+）-3-PPP是一种很好的竞争性σ拮抗剂候选物。

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Evidence against an involvement of the haloperidol-sensitive sigma recognition site in the discriminative stimulus properties of (+)-N-allylnormetazocine ((+)-SKF 10,047).有证据表明，氟哌啶醇敏感的σ识别位点与（+）-N-烯丙基去甲左啡诺（（+）-SKF 10,047）的辨别刺激特性无关。
Br J Pharmacol. 1990 Jan;99(1):145-51. doi: 10.1111/j.1476-5381.1990.tb14668.x.