EFFECT OF FLUORINE SUBSTITUTION ON THE AGONIST SPECIFICITY OF NOREPINEPHRINE

被引：58

作者：

CANTACUZENE, D ^{[1
]}

KIRK, KL ^{[1
]}

MCCULLOH, DH ^{[1
]}

CREVELING, CR ^{[1
]}

机构：

[1] NIAMDD,BIOORGAN CHEM LAB,BETHESDA,MD 20014

来源：

SCIENCE | 1979年 / 204卷 / 4398期

关键词：

D O I：

10.1126/science.221978

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

Substitution of fluorine for hydrogen in position 2, 5, or 6 of the aromatic ring of norepinephrine markedly alters the α- and β-adrenergic agonist properties of norepinephrine. The 6-fluoro isomer is an α-adrenergic agonist with virtually no β agonist activity, while the 2-fluoro isomer is a β-adrenergic agonist with little α activity. The 5-fluoro isomer is equipotent with norepinephrine as an α agonist and significantly more potent as a β agonist. The possible physiochemical basis for these differences is discussed. Copyright © 1979 AAAS.

引用

页码：1217 / 1219

页数：3

共 22 条

[1]

BLASCHKO H, 1972, HDB EXPT PHARMACOLOG, V33, P283

[2] FLUORINATED MOLECULE AS A TRACER - DIFLUOROSEROTONIN IN HUMAN PLATELETS MAPPED BY ELECTRON ENERGY-LOSS SPECTROSCOPY [J].