文章基本信息

标题：フロムワレリル尿素の代謝について(第3報)家兎尿からの2-(Methylthio)-3-methylbutyrylureaの検出および安定同位体希釈法による定量
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作者：礒野秀夫
期刊名称：Journal of Health Science
印刷版ISSN：1344-9702
电子版ISSN：1347-5207
出版年度：1978
卷号：24
期号：1
页码：5-10
DOI：10.1248/jhs1956.24.5
出版社：The Pharmaceutical Society of Japan
摘要：On the way of the study on the metabolism of α-bromoisovalerylurea (BV), a series of new mass fragment ions (m/e 103, 115, 130, 144, 175, and 190) was observed in the mass spectrum of crude extracts from BV-administered rabbit urine. After purification of the extracts by silica gel column chromatography and subsequent thin-layer chromatography (TLC), small pieces of crystals were obtained and characterized to be 2-(methylthio)-3-methylbutyrylurea (BM) by comparison of melting point, Rf value in TLC, mass spectrum, and infrared spectrum with those of the standard BM, synthesized from BV and methylmercaptan. In order to know the amount of BM excreted by the isotope dilution method using a mass spectrometer, 2-(methylthio-d₃)-3-methylbutyrylurea (BMd₃) was synthesized from BV, thiourea, and methyld₃ iodide. After the administration of 1 g of BV to a male rabbit (ca. 3.5kg), approximately 4 mg of BM was found to be excreted in the urine within 30 hr.
关键词：bromvalerylurea;drug metabolism;methylmercaptan derivative;isotope dilution method;hypnotics;urine analysis;excretion;mass spectrometry;deuterium;sulfide