Wood M S, Traynor J R
Department of Chemistry, University of Technology, Loughborough, Leicestershire, England.
J Neurochem. 1989 Jul;53(1):173-8. doi: 10.1111/j.1471-4159.1989.tb07310.x.
The binding of the unselective opioid antagonist [3H]diprenorphine to homogenates prepared from rat brain and from guinea-pig brain and cerebellum has been studied in HEPES buffer containing 10 mM Mg2+ ions. Sequential displacement of bound [3H]diprenorphine by ligands with selectivity for mu-, delta-, and kappa-opioid receptors uncovers the multiple components of binding. In the presence of cold ligands that occupy all mu-, delta-, and kappa-sites, opioid binding still remains. This binding represents 20% of total specific sites and is displaced by naloxone. The nature of these undefined opioid binding sites is discussed.
在含有10 mM镁离子的HEPES缓冲液中，研究了非选择性阿片类拮抗剂[3H]二丙诺啡与大鼠脑、豚鼠脑及小脑匀浆的结合情况。对μ-、δ-和κ-阿片受体具有选择性的配体对结合的[3H]二丙诺啡进行顺序置换，揭示了结合的多个成分。在存在占据所有μ-、δ-和κ-位点的冷配体的情况下，阿片类结合仍然存在。这种结合占总特定位点的20%，并可被纳洛酮置换。讨论了这些未明确的阿片类结合位点的性质。
Zotero 插件