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在哺乳动物大脑中鉴定惊厥性阿片碱蒂巴因。

Identification of the convulsant opiate thebaine in mammalian brain.

作者信息

Kodaira H, Lisek C A, Jardine I, Arimura A, Spector S

机构信息

Roche Institute of Molecular Biology, Roche Research Center, Nutley, NJ 07110.

出版信息

Proc Natl Acad Sci U S A. 1989 Jan;86(2):716-9. doi: 10.1073/pnas.86.2.716.

DOI:10.1073/pnas.86.2.716
PMID:2911601
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC286545/
Abstract

The convulsant opiate thebaine, an intermediate of morphine biosynthesis, was purified from bovine brain to homogeneity by gel filtration and high-performance liquid chromatography (HPLC) monitored by a radioimmunoassay. The immunoreactive material behaved identically to standard thebaine in two HPLC systems and was confirmed to be thebaine by combined gas chromatography/mass spectrometry. To our knowledge, the presence of thebaine in mammalian tissue has not been demonstrated previously. Codeine and morphine were also found to exist in ovine brain. The presence of thebaine in ovine brain provides strong evidence that morphine and codeine, in various mammalian tissues, are of endogenous origin and actually biosynthesized from a precursor.

摘要

惊厥性阿片碱蒂巴因是吗啡生物合成的中间体,通过凝胶过滤和高效液相色谱(HPLC)从牛脑中纯化至同质,并用放射免疫测定法进行监测。在两个HPLC系统中,免疫反应性物质的行为与标准蒂巴因相同,通过气相色谱/质谱联用确认为蒂巴因。据我们所知,此前尚未在哺乳动物组织中证实蒂巴因的存在。在羊脑中也发现了可待因和吗啡。羊脑中存在蒂巴因提供了有力证据,表明在各种哺乳动物组织中,吗啡和可待因是内源性的,实际上是由前体生物合成的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2052/286545/e8b5234e9d19/pnas00242-0319-d.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2052/286545/ce1ae925cfa6/pnas00242-0319-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2052/286545/494fe794cd2f/pnas00242-0319-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2052/286545/b92f29a86173/pnas00242-0319-c.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2052/286545/e8b5234e9d19/pnas00242-0319-d.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2052/286545/ce1ae925cfa6/pnas00242-0319-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2052/286545/494fe794cd2f/pnas00242-0319-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2052/286545/b92f29a86173/pnas00242-0319-c.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2052/286545/e8b5234e9d19/pnas00242-0319-d.jpg

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INVESTIGATIONS ON THE BIOSYNTHESIS OF MORPHINE ALKALOIDS.吗啡生物碱生物合成的研究
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Opiate alkaloids antagonize postsynaptic glycine and GABA responses: correlation with convulsant action.阿片生物碱拮抗突触后甘氨酸和GABA反应:与惊厥作用的相关性。
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Studies on the excitatory and inhibitory influence of intracerebroventricularly injected opioids on seizure thresholds in rats.脑室内注射阿片类药物对大鼠癫痫发作阈值的兴奋和抑制作用的研究。
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Pro- and anticonvulsant actions of morphine and the endogenous opioids: involvement and interactions of multiple opiate and non-opiate systems.吗啡及内源性阿片类物质的促惊厥与抗惊厥作用:多种阿片类和非阿片类系统的参与及相互作用
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Antagonism of the spinal cord effects of morphine and cyclazocine by naloxone and thebaine.纳洛酮和蒂巴因对吗啡及环唑辛脊髓效应的拮抗作用。
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