6-[18F]fluorometaraminol: a radiotracer for in vivo mapping of adrenergic nerves of the heart.
6-[18F]fluorometaraminol: a radiotracer for in vivo mapping of adrenergic nerves of the heart.
复制标题
6-[18F]氟间氨基酚：一种用于心脏肾上腺素能神经体内绘图的放射性示踪剂。
DOI：
10.1021/jm00397a016
复制
发表时间：
1988
影响因子：
7.3
通讯作者：
Toorongian,SA
中科院分区：
文献类型：
--
作者：
Mislankar,SG;Gildersleeve,DL;Wieland,DM;Massin,CC;Mulholland,GK;Toorongian,SA
The false neurotransmitter metaraminol has been 18F labeled and evaluated as a possible heart imaging agent on the basis of its selective accumulation in adrenergic nerves. Reaction of 6-(acetoxymercurio)-jV-t-BOC-metaraminol with acetyl hypofluorite followed by removal of the BOC group provides a regiospecifiq synthesis of 6-fluorometaraminol (4). Use of acetyl hypo [18F] fluorite gives [18F]-4 in 60 min in 20-42% radiochemical yield. Systemicblockade of the neuronal uptake-1 carrierwith desmethylimipramine or systemic destruction Of the adrenergic nerves with 6-hydroxydopamine lowers [18F]-4 accumulation> 85% in all four regions of the rat heart. These preliminary findings suggest that [18F]-4 could be used to aásess neuronal damage in various heart diseases by positron emission tomography.Metaraminol is a substitute adrenergic transmitter that stoichiometrically displaces norepinephrine (NE) from its storage sites within the neuron. 2 Like NE, metaraminol is transported into the adrenergic neuron by the uptake-1 carrier protein, sequestered within storage vesicles, and released by nerve impulse. 3 Metaraminol is less potent
