Janković B D, Radulović J
Immunology Research Center, Belgrade, Yugoslavia.
Immunopharmacology. 1994 Sep-Oct;28(2):105-12. doi: 10.1016/0162-3109(94)90026-4.
To investigate the role of brain opioid receptors in immune reactions, quaternary naltrexone (QNtx), a nonselective opioid antagonist which does not cross the brain-blood barrier, was tested for its immunomodulatory activity and ability to antagonize immunological changes produced by centrally applied delta-receptor agonist methionine-enkephalin (Met-Enk) and kappa-opioid receptor agonist MR 2034. Plaque-forming cell (PFC) response served as an immunological model. For this purpose, different groups of Wistar rats were centrally (intracerebroventricularly, i.c.v.) and peripherally (intraperitoneally, i.p., or subcutaneously, s.c.) treated with different doses of Met-Enk. MR 2034 and QNtx. Centrally injected Met-Enk and MR 2034 induced a dose-dependent potentiation and suppression of PFC response, respectively. Small amounts of i.c.v. given QNtx produced a dose-dependent increase in the number of PFC, whereas peripherally administered antagonist potentiated immune response in a dose-independent manner. A dose of 10 micrograms/kg of QNtx given i.c.v. completely abolished the immunopotentiation by Met-Enk. However, a large dose of 5 mg/kg of QNtx given s.c., did not affect the Met-Enk-induced immunoenhancement. Immunosuppression produced by i.c.v. injected MR 2034 was totally abrogated by prior i.c.v. application of QNtx, but partially blocked by s.c. administration of the antagonist.(ABSTRACT TRUNCATED AT 250 WORDS)
为研究脑阿片受体在免疫反应中的作用，对季铵型纳曲酮（QNtx）进行了检测，它是一种不透过血脑屏障的非选择性阿片拮抗剂，检测其免疫调节活性以及拮抗中枢给予的δ受体激动剂甲硫氨酸脑啡肽（Met-Enk）和κ阿片受体激动剂MR 2034所产生的免疫变化的能力。空斑形成细胞（PFC）反应作为一种免疫模型。为此，将不同组的Wistar大鼠分别通过中枢（脑室内，i.c.v.）和外周（腹腔内，i.p.，或皮下，s.c.）给予不同剂量的Met-Enk、MR 2034和QNtx。中枢注射的Met-Enk和MR 2034分别诱导了PFC反应的剂量依赖性增强和抑制。脑室内给予少量QNtx可使PFC数量呈剂量依赖性增加，而外周给予拮抗剂则以非剂量依赖性方式增强免疫反应。脑室内给予10微克/千克剂量的QNtx可完全消除Met-Enk引起的免疫增强作用。然而，皮下给予5毫克/千克的大剂量QNtx并不影响Met-Enk诱导的免疫增强作用。脑室内注射MR 2034所产生的免疫抑制作用可被预先脑室内给予QNtx完全消除，但皮下给予拮抗剂则可部分阻断该作用。（摘要截短于250字）
