Coccini T, Costa L G, Manzo L, Candura S M, Iapadre N, Balestra B, Tonini M
Department of Internal Medicine and Therapeutics, University of Pavia, Italy.
Eur J Pharmacol. 1991 May 30;198(1):105-8. doi: 10.1016/0014-2999(91)90570-g.
In the longitudinal muscle-myenteric plexus preparation (LMMP) of the guinea-pig ileum, the non-opioid sigma receptors agonists, 1,3-di-ortho-tolylguanidine (DTG) and (+)N-allyl-N-normetazocine [(+)SKF 10,047], had opposite effects on nerve-mediated cholinergic contractions caused by electrical field stimulation. DTG (0.1-10 microM) inhibited and (+)SKF 10,047 (0.1-10 microM) markedly enhanced these contractile responses. Both effects were evaluated in the presence (0.5 or 1 microM) of the putative antagonists at central sigma sites: haloperidol, rimcazole, BMY 14802 and dextromethorphan. Haloperidol and dextromethorphan were ineffective. Rimcazole antagonized the effect of both DTG and (+)SKF 10.047. BMY 14802 antagonized the (+)SKF 10.047-mediated excitatory response only. These results suggest that two sigma receptor subtypes are present in enteric cholinergic motor neurons innervating the longitudinal coat. Rimcazole and BMY 14802 may provide useful tools for the characterization of peripheral non-opioid sigma receptors.
在豚鼠回肠的纵行肌-肠肌丛标本（LMMP）中，非阿片类σ受体激动剂1,3-二邻甲苯基胍（DTG）和（+）N-烯丙基-N-去甲左啡诺[（+）SKF 10,047]，对电场刺激引起的神经介导的胆碱能收缩有相反的作用。DTG（0.1 - 10微摩尔）抑制，而（+）SKF 10,047（0.1 - 10微摩尔）显著增强这些收缩反应。在存在中枢σ位点假定拮抗剂（0.5或1微摩尔）：氟哌啶醇、利姆卡唑、BMY 14802和右美沙芬的情况下评估了这两种作用。氟哌啶醇和右美沙芬无效。利姆卡唑拮抗DTG和（+）SKF 10.047的作用。BMY 14802仅拮抗（+）SKF 10.047介导的兴奋反应。这些结果表明，支配纵行肌层的肠胆碱能运动神经元中存在两种σ受体亚型。利姆卡唑和BMY 14802可能为外周非阿片类σ受体的特性研究提供有用的工具。
