氯苯丁胺在人体中的代谢、分布及排泄
The metabolism, distribution and elimination of chlorphentermine in man.
作者信息
Beckett A H, Bélanger P M
出版信息
Br J Clin Pharmacol. 1977 Apr;4(2):193-200. doi: 10.1111/j.1365-2125.1977.tb00693.x.
Abstract
1 A gas-liquid chromatography procedure for the determination of chlorphentermine (I), N-hydroxychlorphentermine (II) and alpha,alpha-dimethyl-alpha-nitro-beta-(4-chlorophenyl)ethane (IV) in urine has been developed. Also methods are reported to determine conjugated II and the total N-oxidized metabolites of I, i.e. II, conjugated II, alpha,alpha-dimethyl-alpha-nitroso-beta-(4-chlorophenyl)ethane (III) and IV in urine. 2 The synthesis of alpha,alpha-dimethyl-alpha-nitroso-beta-(4-chlorophenyl)ethane (III) and its properties are reported. 3 The kinetics of urinary excretion of I and its metabolic products after the oral administration of I to a human subject on separate occasions have been studied. Under normal conditions of urinary pH, metabolism by N-oxidation was the main elimination route of I; acidifying the urine increased the urinary excretion of unchanged I at the expense of the N-oxidized products. 4 The importance of the N-oxidation metabolic route in the distribution of chlorphentermine (I) in man is discussed.
摘要
- 已开发出一种气相色谱法，用于测定尿液中的氯苯丁胺（I）、N-羟基氯苯丁胺（II）和α,α-二甲基-α-硝基-β-(4-氯苯基)乙烷（IV）。还报道了测定尿液中结合态II以及I的总N-氧化代谢物（即II、结合态II、α,α-二甲基-α-亚硝基-β-(4-氯苯基)乙烷（III）和IV）的方法。2. 报道了α,α-二甲基-α-亚硝基-β-(4-氯苯基)乙烷（III）的合成及其性质。3. 研究了在不同时间给人体受试者口服I后，I及其代谢产物的尿排泄动力学。在正常尿液pH条件下，N-氧化代谢是I的主要消除途径；酸化尿液会增加未变化的I的尿排泄量，同时减少N-氧化产物的排泄量。4. 讨论了N-氧化代谢途径在氯苯丁胺（I）在人体分布中的重要性。
相似文献
1
The metabolism, distribution and elimination of chlorphentermine in man.氯苯丁胺在人体中的代谢、分布及排泄
Br J Clin Pharmacol. 1977 Apr;4(2):193-200. doi: 10.1111/j.1365-2125.1977.tb00693.x.
2
Species variations in the N-oxidation of chlorphentermine.氯苯丁胺N-氧化反应中的物种差异。
Biochem Pharmacol. 1975 Dec 15;24(24):2225-32. doi: 10.1016/0006-2952(75)90259-2.
3
The reversibility of N-oxidation in vivo. The fate of 14C-N-hydroxychlorphentermine and 14C-nitrochlorphentermine in the rat.体内N-氧化的可逆性。大鼠体内14C-N-羟基氯苯丙胺和14C-硝基氯苯丙胺的归宿。
Biochem Pharmacol. 1980 May 15;29(10):1325-30. doi: 10.1016/0006-2952(80)90425-6.
4
The disposition of phentermine and its N-oxidized metabolic products in the rabbit.
Xenobiotica. 1978 Jan;8(1):55-60. doi: 10.3109/00498257809060383.
5
Metabolism of chlorphentermine and phentermine in man to yield hydroxylamino, C-nitroso- and nitro-compounds.氯苯丁胺和苯丁胺在人体内的代谢产生羟胺、C-亚硝基和硝基化合物。
J Pharm Pharmacol. 1974 Mar;26(3):205-6. doi: 10.1111/j.2042-7158.1974.tb09256.x.
6
The reversibility of the N-oxidation of chlorphentermine in vivo [proceedings].氯苯丁胺体内N-氧化反应的可逆性[会议论文集]
Biochem Soc Trans. 1977;5(4):1005-6. doi: 10.1042/bst0051005.
7
Inhibition of chlorphentermine binding in rat lung: application of connectivity theory.氯苯丁胺在大鼠肺中的结合抑制：连通性理论的应用
Life Sci. 1980 Sep 22;27(12):1041-6. doi: 10.1016/0024-3205(80)90027-2.
8
The metabolism and urinary excretion in man of phentermine, and the influence of N-methyl and p-chloro-substitution.苯丁胺在人体中的代谢及尿排泄，以及N-甲基和对氯取代的影响。
J Pharm Pharmacol. 1971 Apr;23(4):288-94. doi: 10.1111/j.2042-7158.1971.tb08659.x.
9
Effect of desmethylimipramine on tissue distribution and anorectic activity of chlorphentermine in rats.
Life Sci. 1981 Apr 27;28(17):1931-8. doi: 10.1016/0024-3205(81)90301-5.
10
Effect of desmethylimipramine on the kinetics of chlorphentermine accumulation in isolated perfused rat lung.
J Pharmacol Exp Ther. 1979 Dec;211(3):514-8.
引用本文的文献
1
Synthesis of Phentermine and its Derivatives.苯丁胺及其衍生物的合成。
Curr Org Synth. 2024;21(5):583-594. doi: 10.2174/1570179420666230530095245.
2
Synthesis and evaluation of N-isopropyl-p-[C]methylamphetamine as a novel cerebral blood flow tracer for positron emission tomography.N-异丙基-p-[C]甲基苯丙胺作为一种新型正电子发射断层显像脑血流示踪剂的合成与评价
EJNMMI Res. 2020 Oct 1;10(1):115. doi: 10.1186/s13550-020-00702-5.
3
Clinical pharmacokinetics of amfetamine and related substances: monitoring in conventional and non-conventional matrices.苯丙胺及相关物质的临床药代动力学：常规和非常规基质中的监测
Clin Pharmacokinet. 2004;43(3):157-85. doi: 10.2165/00003088-200443030-00002.
本文引用的文献
1
Blood levels of chlorphentermine in man.人体中氯苯丁胺的血液水平。
J Pharm Sci. 1970 Mar;59(3):306-9. doi: 10.1002/jps.2600590305.
2
Distribution and metabolism of chlorphentermine-C14 in rats and mice.
Biochem Pharmacol. 1968 Jul;17(7):1243-50. doi: 10.1016/0006-2952(68)90061-0.
3
Microsomal N-hydroxylation of phenylalkylamines. Identification of N-hydroxylated phenylalkylamines as their trimethylsilyl derivatives by GC-Ms.
Acta Pharm Suec. 1973 Dec;10(6):493-506.
4
Long-term effects of N-hydroxy-4-chloroamphetamine on the level and accumulation of 5-hydroxytryptamine in the rat brain.
Eur J Pharmacol. 1974 Sep;28(1):222-4. doi: 10.1016/0014-2999(74)90136-8.
5
The identification of three new metabolic products of phentermine after liver microsomal incubation.肝脏微粒体孵育后苯丁胺三种新代谢产物的鉴定。
Xenobiotica. 1974 Aug;4(8):509-19. doi: 10.3109/00498257409052103.
6
The metabolism and urinary excretion in man of phentermine, and the influence of N-methyl and p-chloro-substitution.苯丁胺在人体中的代谢及尿排泄，以及N-甲基和对氯取代的影响。
J Pharm Pharmacol. 1971 Apr;23(4):288-94. doi: 10.1111/j.2042-7158.1971.tb08659.x.
7
The relation between blood levels and urinary excretion of amphetamine under controlled acidic and under fluctuating urinary pH values using [14C] amphetamine.使用[14C]苯丙胺，在尿液pH值受控呈酸性以及尿液pH值波动的情况下，苯丙胺血液水平与尿液排泄之间的关系。
J Pharm Pharmacol. 1969 Apr;21(4):251-8. doi: 10.1111/j.2042-7158.1969.tb08241.x.
8
A note on spectrophotometric methods for the determination of norethynodrel and mestranol in tablets.关于片剂中炔诺酮和炔雌醇甲醚分光光度测定方法的说明
J Pharm Pharmacol. 1967 Jan;19(1):41-4. doi: 10.1111/j.2042-7158.1967.tb07991.x.
9
Urinary excretion kinetics of amphetamine in man.
J Pharm Pharmacol. 1965 Oct;17(10):628-39. doi: 10.1111/j.2042-7158.1965.tb07575.x.
10
Drug-induced phospholipidosis.
Ger Med. 1973 Winter;3(3-4):128-35.
Zotero 插件