Dragatsis I, Papazafiri P, Zioudrou C, Gerozissis K
Institute of Biology, National Centre for Scientific Research, Demokritos, Attiki, Greece.
J Endocrinol. 1995 May;145(2):263-70. doi: 10.1677/joe.0.1450263.
It is currently accepted that opioids modify the secretion of LH by affecting the release of GnRH in the hypothalamus. A direct action of opioids at the pituitary level is not yet fully established. To this end, we tested the effects of opioids on the release of LH by the entire pituitary in adult male rats. Opioid agonists with mu (DAGO), delta (DS-LET) and kappa (U-50488H) specificity were tested at 0.01 to 10 microM in static incubations. DAGO inhibited dose-dependently the spontaneous and GnRH-induced release of LH. DSLET inhibited only the GnRH-induced release of LH. On the other hand, U-50488H increased spontaneous LH release dose-dependently. The opioid antagonists naloxone, diallyl-G (delta antagonist) and MR 2266 (kappa antagonist) blocked the effects induced by DAGO, DSLET or U-50488H respectively, implying an opioid receptor-mediated effect. The above results showed that opioids with mu, delta and kappa specificity act on the entire pituitary and modify differentially the release of LH. In this study we also compared spontaneous and GnRH-induced LH release by anterior and entire pituitaries and found that the amount of LH released by the anterior lobe was twofold higher, suggesting that inhibitory factors present in the neurointermediate part may affect the release of LH.
目前人们认为,阿片类药物通过影响下丘脑促性腺激素释放激素(GnRH)的释放来改变促黄体生成素(LH)的分泌。阿片类药物在垂体水平的直接作用尚未完全明确。为此,我们测试了阿片类药物对成年雄性大鼠整个垂体释放LH的影响。在静态孵育中,以0.01至10微摩尔的浓度测试了具有μ(DAGO)、δ(DS - LET)和κ(U - 50488H)特异性的阿片类激动剂。DAGO剂量依赖性地抑制LH的自发释放和GnRH诱导的释放。DSLET仅抑制GnRH诱导的LH释放。另一方面,U - 50488H剂量依赖性地增加LH的自发释放。阿片类拮抗剂纳洛酮、二烯丙基 - G(δ拮抗剂)和MR 2266(κ拮抗剂)分别阻断了DAGO、DSLET或U - 50488H诱导的效应,这意味着存在阿片受体介导的效应。上述结果表明,具有μ、δ和κ特异性的阿片类药物作用于整个垂体,并以不同方式改变LH的释放。在本研究中,我们还比较了前叶垂体和整个垂体的LH自发释放和GnRH诱导释放情况,发现前叶释放的LH量高出两倍,这表明神经中间部存在的抑制因子可能会影响LH的释放。