N-（5-吡咯烷基戊-3-炔基）-琥珀酰亚胺（BL 14）体外代谢过程中炔基α位的酶促氧化作用。
Enzymic oxidation alpha to the acetylenic group in the metabolism of N-(5-pyrrolidinopent-3-ynyl)-succinimide (BL 14) in vitro.
作者信息
Lindeke B, Hallström G, Anderson E
出版信息
Xenobiotica. 1978 Jun;8(6):341-8. doi: 10.3109/00498257809070017.
PMID:676341
Abstract
- The product of alpha-acetylenic oxidation of N-(5-pyrrolidinopent-3-ynyl)-succinimide (BL 14) by rat liver preparations was identified as N-(5-pyrrolidino-2-hydroxypent-3-ynyl)succinimide, by mass spectral analysis of metabolites of deuterium-labelled and non-labelled substrate. 2. The synthesis and physicochemical characteristics of the metabolite are reported. 3. Substantial amounts of the metabolite were obtained in preparations from phenobarbital-treated rats, while only minute amounts were formed by non-induced preparations. 4. Evidence for the involvement of an inducible cytochrome P-450 system in effecting this alpha-acetylenic oxidation is presented.
摘要
- 通过对氘标记和未标记底物的代谢产物进行质谱分析，大鼠肝脏制剂对N-(5-吡咯烷基戊-3-炔基)琥珀酰亚胺（BL 14）进行α-乙炔氧化的产物被鉴定为N-(5-吡咯烷基-2-羟基戊-3-炔基)琥珀酰亚胺。2. 报道了该代谢产物的合成及其物理化学特性。3. 从苯巴比妥处理的大鼠的制剂中获得了大量的该代谢产物，而未诱导的制剂仅形成微量产物。4. 提供了关于诱导型细胞色素P-450系统参与这种α-乙炔氧化作用的证据。
相似文献
1
Enzymic oxidation alpha to the acetylenic group in the metabolism of N-(5-pyrrolidinopent-3-ynyl)-succinimide (BL 14) in vitro.N-（5-吡咯烷基戊-3-炔基）-琥珀酰亚胺（BL 14）体外代谢过程中炔基α位的酶促氧化作用。
Xenobiotica. 1978 Jun;8(6):341-8. doi: 10.3109/00498257809070017.
2
Metabolism of N-(5-pyrrolidinopent-3-ynyl)-succinimide (BL 14) in rat liver preparations. Characterization of four oxidative reactions.N-(5-吡咯烷基戊-3-炔基)-琥珀酰亚胺（BL 14）在大鼠肝脏制剂中的代谢。四种氧化反应的表征
Xenobiotica. 1981 Jul;11(7):459-71. doi: 10.3109/00498258109045856.
3
Metabolic N-oxidation of alpha-acetylenic amines-a gas chromatographic mass spectrometric investigation of the chemical decomposition of N-(5-pyrrolidinopent-3-ynyl)succinimide N'-oxide using deuterium substitution.α-炔丙基胺的代谢N-氧化——使用氘代对N-(5-吡咯烷基戊-3-炔基)琥珀酰亚胺N'-氧化物化学分解的气相色谱-质谱研究
Biomed Mass Spectrom. 1981 Oct;8(10):514-20. doi: 10.1002/bms.1200081010.
4
Synthesis and mass spectrometric investigations of metabolites of N-(5-pyrrolidino-pent-3-ynyl)succinimide (BL 14).
Acta Pharm Suec. 1980;17(1):31-54.
5
Metabolism of antiparkinson agent dopazinol by rat liver microsomes.
Drug Metab Dispos. 1990 Nov-Dec;18(6):1025-30.
6
Reductive metabolism of an alpha,beta-ketoalkyne, 4-phenyl-3-butyn-2-one, by rat liver preparations.
Drug Metab Dispos. 2002 Apr;30(4):414-20. doi: 10.1124/dmd.30.4.414.
7
A new pathway for the oxidative metabolism of chloramphenicol by rat liver microsomes.大鼠肝脏微粒体对氯霉素进行氧化代谢的新途径。
Drug Metab Dispos. 1982 Sep-Oct;10(5):439-45.
8
In vitro metabolic N- and C-oxidation of phenanthridine.菲啶的体外代谢N-氧化和C-氧化
Eur J Drug Metab Pharmacokinet. 1997 Oct-Dec;22(4):345-9. doi: 10.1007/BF03190969.
9
Spin trapping of a free radical intermediate formed during microsomal metabolism of hydrazine.肼微粒体代谢过程中形成的自由基中间体的自旋捕获。
Biochem Biophys Res Commun. 1985 Dec 31;133(3):1086-91. doi: 10.1016/0006-291x(85)91247-1.
10
The metabolism of antifertility steroids. The in virto metabolism of chlormadinone acetate.抗生育甾体的代谢。醋酸氯地孕酮的体外代谢。
Drug Metab Dispos. 1974 May-Jun;2(3):214-20.
引用本文的文献
1
The metabolic oxidation of the ethynyl group in 4-ethynylbiphenyl in vitro.4-乙炔基联苯中乙炔基在体外的代谢氧化。
Biochem J. 1980 Jun 15;188(3):867-72. doi: 10.1042/bj1880867.
2
Metabolic activation of acetylenes. Covalent binding of [1,2-14C]octyne to protein, DNA and haem in vitro and the protective effects of certain thiol compounds.乙炔的代谢活化。[1,2-¹⁴C]辛炔在体外与蛋白质、DNA和血红素的共价结合以及某些硫醇化合物的保护作用。
Biochem J. 1984 May 15;220(1):85-94. doi: 10.1042/bj2200085.
Zotero 插件