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Effects of Aminoadamantane Derivatives on Morphine-Induced Analgesia in Mice
Pharmaceutical Chemistry Journal ( IF 0.9 ) Pub Date : 2020-07-01 , DOI: 10.1007/s11094-020-02202-1
L. G. Kolik , A. V. Nadorova , I. V. Chernyakova , E. A. Val’dman

The effects of low-affinity NMDA-receptor antagonists amantadine (1-aminoadamantane hydrochloride) and hemantane [N-(2-adamantyl)hexamethyleneimine hydrochloride] on morphine-induced analgesia in C57Bl/6 mice were studied. Amantadine (10 and 20 mg/kg, i.p.) per se did not affect the latent period of the response in the hot-plate test while hemantane (10 and 20 mg/kg, i.p.) increased dose-dependently pain thresholds 180 and 240 min after administration. Morphine (20 mg/kg, s.c.) showed a time—effect dependence (30 – 120 min). The aminoadamantanes were administered 90 min after the opioid to assess their effects on morphine-induced antinociception. The responses of the animals were recorded for the next 2.5 h. The aminoadamantanes potentiated and extended the analgesic activity of morphine in the order of efficacy amantadine < hemantane. The results indicated that the aminoadamantanes had different capabilities to cause delayed analgesia and modulated opioid antinociceptive activity at the supraspinal level.

中文翻译:

氨基金刚烷衍生物对吗啡诱导小鼠镇痛的影响

研究了低亲和力 NMDA 受体拮抗剂金刚烷胺(1-氨基金刚烷盐酸盐)和金刚烷 [N-(2-金刚烷基)六亚甲基亚胺盐酸盐]对 C57Bl/6 小鼠吗啡诱导的镇痛作用的影响。金刚烷胺(10 和 20 毫克/公斤,腹腔注射)本身不影响热板试验中反应的潜伏期,而金刚烷(10 和 20 毫克/公斤,腹腔注射)则增加剂量依赖性疼痛阈值 180 和 240 分钟给药后。吗啡 (20 mg/kg, sc) 显示出时间效应依赖性(30 – 120 分钟)。氨基金刚烷在阿片类药物后 90 分钟给药,以评估它们对吗啡诱导的镇痛作用的影响。在接下来的 2.5 小时内记录动物的反应。氨基金刚烷以金刚烷胺 < 金刚烷的功效顺序增强和延长吗啡的镇痛活性。
更新日期:2020-07-01
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