THE IRREVERSIBLE NARCOTIC ANTAGONISTIC AND REVERSIBLE AGONISTIC PROPERTIES OF THE FUMARAMATE METHYL-ESTER DERIVATIVE OF NALTREXONE
THE IRREVERSIBLE NARCOTIC ANTAGONISTIC AND REVERSIBLE AGONISTIC PROPERTIES OF THE FUMARAMATE METHYL-ESTER DERIVATIVE OF NALTREXONE
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DOI：
10.1016/0014-2999(81)90355-1
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发表时间：
1981-01-01
影响因子：
5
通讯作者：
PORTOGHESE, PS
中科院分区：
文献类型：
--
作者：
TAKEMORI, AE;LARSON, DL;PORTOGHESE, PS
度量。纳曲酮（. β .- fna）和羟吗啡酮（. β .- fna）的-富马马酸甲酯衍生物。在豚鼠回肠纵肌制剂中，发现两者都是可逆的激动剂。-FNA对吗啡具有不可逆的拮抗作用；度量。-FOA没有这种能力。pA2[激动剂对拮抗剂的有效浓度]值分析显示。-FOA类似于单纯的激动剂，如吗啡和脑啡肽。-FNA类似于混合激动-拮抗剂如纳洛啡和戊唑嗪。拮抗作用。-FNA具有很强的选择性，因为它可以拮抗纯激动剂，但对混合激动剂-拮抗剂、乙基酮环唑辛或其他非阿片类激动剂（如去甲肾上腺素）的作用几乎没有影响。
The .beta.-fumaramate methyl ester derivatives of naltrexone (.beta.-FNA) and oxymorphone (.beta.-fluoro-orotic acid) were both found to be reversible agonists on the guinea pig ileal longitudinal muscle preparation. .beta.-FNA possessed an irreversible antagonistic effect against morphine; .beta.-FOA had no such capacity. Analysis by pA2 [effective concentration of agonist to antagonist] values revealed that .beta.-FOA resembled pure agonists like morphine and enkephalin while .beta.-FNA resembled the mixed agonist-antagonists like nalorphine and pentazocine. The antagonism by .beta.-FNA was very selective in that it antagonized pure agonists but had little or no effect on the effects of either mixed agonist-antagonists, ethylketocyclazocine or other non-opiate-type agonists like norepinephrine.