Pharmacological characterization in vivo of the novel opiate, beta-funaltrexamine.
Pharmacological characterization in vivo of the novel opiate, beta-funaltrexamine.
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发表时间：
1982-03
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通讯作者：
S. Ward;P. Portoghese;A. Takemori
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作者：
S. Ward;P. Portoghese;A. Takemori
研究了β-富纳曲胺（β-FNA）（纳曲酮的富马酸甲酯衍生物）在体内抗伤害测试中的作用概况。 Beta-FNA 表现出持续时间短的抗伤害作用，并且似乎是由 kappa 受体相互作用介导的。相比之下，β-FNA 的拮抗作用持续时间非常长，并且对 nu 激动剂相互作用具有选择性。该作用概况与 β-FNA 的体外作用概况一致。 β-FNA 对 mu 介导作用的选择性持久拮抗作用可能对于阐明多种阿片受体功能具有重要价值。
The profile of action of beta-funaltrexamine (beta-FNA), the fumaramate methyl ester derivative of naltrexone, on antinociceptive tests in vivo was investigated. Beta-FNA demonstrated antinociceptive actions that were of short duration and that appeared to be mediated by kappa receptor interaction. In contrast, the antagonist actions of beta-FNA were of remarkably long duration and were selective toward nu agonist interactions. This profile of action is consistent with the profile of action of beta-FNA in vitro. The selective long-lasting antagonism of mu-mediated effects by beta-FNA may be of great value in the elucidation of multiple opioid receptor function.