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大鼠脑提取物中6-甲氧基-1,2,3,4-四氢-β-咔啉的区域形成

Regional formation of 6-methoxy-1,2,3,4-tetrahydro-beta-carboline in rat brain extract.

作者信息

Hsu L L, Mandell A J

出版信息

Res Commun Chem Pathol Pharmacol. 1975 Oct;12(2):355-62.

PMID:1197918
Abstract

In the presence of 5-methoxytryptamine (5-MeOT), 5-methyltetrahydrofolic acid (5-MTHF) yields 6-methoxy-1,2,3,4-tetrahydro-beta-carboline (6-MeOTHbetaC) in rat brain extracts, possibly via formaldehyde formation catalyzed by methylenetetrahydrofolate reductase. The formation of 6-MeOTHbetaC in selected brain regions, ranging from 452 +/- 40 pmol formed per mg protein per hour in corpus striatum to 119 +/- 17 pmol in cingulate cortex, is significantly correlated with the regional distribution of 1,2,3,4-tetrahydro-beta-carboline (THbetaC) formed from 5-MTHF and tryptamine (r = 0.76, p less than 0.01) as well as that of methylene-beta-phenylethylimine (MbetaphiEI) from 5-MTHF and beta-phenylethylamine (betaphiEA; r = 0.90, p less than 0.01). FAD enhances the activity, lowering both Vmax and Km values with respect to 5-MeOT and Vmax, but not Km, with respect to 5-MTHF.

摘要

在大鼠脑提取物中,5-甲氧基色胺(5-MeOT)存在的情况下,5-甲基四氢叶酸(5-MTHF)可能通过亚甲基四氢叶酸还原酶催化生成甲醛,进而产生6-甲氧基-1,2,3,4-四氢-β-咔啉(6-MeOTHβC)。在选定的脑区中,6-MeOTHβC的生成量从纹状体中每毫克蛋白质每小时生成452±40皮摩尔到扣带回皮质中119±17皮摩尔不等,与由5-MTHF和色胺生成的1,2,3,4-四氢-β-咔啉(THβC)的区域分布显著相关(r = 0.76,p < 0.01),也与由5-MTHF和β-苯乙胺(β-phiEA)生成的亚甲基-β-苯乙亚胺(MbetaphiEI)的区域分布显著相关(r = 0.90,p < 0.01)。黄素腺嘌呤二核苷酸(FAD)增强了该活性,降低了相对于5-MeOT的Vmax和Km值以及相对于5-MTHF的Vmax,但不降低Km值。

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