SYNTHESIS AND BIOLOGICAL EVALUATION OF 14-ALKOXYMORPHINANS .9. 14-O-ETHYL-5-METHYLNALTREXONE, AN OPIOID ANTAGONIST WITH UNUSUAL SELECTIVITY

被引：10

作者：

SCHMIDHAMMER, H ^{[1
]}

SCHRATZ, A ^{[1
]}

SCHMIDT, C ^{[1
]}

PATEL, D ^{[1
]}

TRAYNOR, JR ^{[1
]}

机构：

[1] LOUGHBOROUGH UNIV TECHNOL, DEPT CHEM, LOUGHBOROUGH LE11 3TU, LEICS, ENGLAND

来源：

HELVETICA CHIMICA ACTA | 1993年 / 76卷 / 01期

关键词：

D O I：

10.1002/hlca.19930760131

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

14-O-Ethyl-5-methylnaloxone (7) and 14-O-ethyl-5-methylnaltrexone (8) have been prepared starting from 14-O-ethyl-5-methyloxycodone (9) in several steps. Both, 7 and 8, were found to be opioid antagonists in vitro and in vivo. Compound 7 exhibited some selectivity for mu opioid receptors, whereas compound 8 did not show selectivity for any of the receptor types. In the AcOH-writhing antagonism test, 8 was not able to antagonize morphine-induced antinociception, but antagonized fentanyl- and sufentanil-induced antinociception.

引用

页码：476 / 480

页数：5

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