Feigenbaum J J, Simantov R
Department of Research and Development, American Institute of Biotechnology, Illinois, IL 60007-3840, USA.
Neurosci Lett. 1996 Jul 5;212(1):5-8. doi: 10.1016/0304-3940(96)12786-5.
gamma-Hydroxybutyrate (GHB) and morphine induce a number of similar effects. Moreover, the effects they elicit can be reversed by the opiate antagonist naloxone (NX), suggesting that GHB may produce at least some of its central effects by acting as an opiate agonist. The present study considered this possibility by examining the effect of GHB on mu, delta, and kappa-opioid receptor binding in concentrations of 1 nM-0.1 mM. GHB was inactive in each instance, at every dose examined. GHB is consequently not a direct opiate receptor agonist. It is also unlikely to be an indirect (enkephalin or dynorphin release-stimulating) agonist. The mechanism of action involved whereby NX can reverse the effects of GHB must therefore not involve opioid mechanisms; at least not directly.
γ-羟基丁酸（GHB）和吗啡会引发一些相似的效应。此外，它们所引发的效应可被阿片类拮抗剂纳洛酮（NX）逆转，这表明GHB可能至少部分通过作为阿片类激动剂来产生其某些中枢效应。本研究通过检测浓度为1 nM至0.1 mM的GHB对μ、δ和κ阿片受体结合的影响来探讨这种可能性。在所检测的每个剂量下，GHB在每种情况下均无活性。因此，GHB不是直接的阿片受体激动剂。它也不太可能是间接（刺激脑啡肽或强啡肽释放）激动剂。因此，NX能够逆转GHB效应所涉及的作用机制必定不涉及阿片类机制；至少不是直接涉及。
