6-[18F]fluorometaraminol. A radiotracer for in vivo mapping of adrenergic nerves of the heart
作者:Suresh G. Mislankar、David L. Gildersleeve、Donald M. Wieland、Christopher C. Massin、G. Keith Mulholland、Steven A. Toorongian
DOI:10.1021/jm00397a016
日期:1988.2
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)-N-t-BOC-metaraminol with acetyl hypofluorite followed by removal of the BOC group provides a regiospecific synthesis of 6-fluorometaraminol (4). Use of acetyl hypo[18F]fluorite gives [18F]-4 in 60 min in 20-42% radiochemical yield. Systemic blockade of the neuronal uptake-1 carrier with desmethylimipramine or systemic destruction of the adrenergic nerves with 6-hydroxydopamine lowers [18F]-4 accumulation greater than or equal to 85% in all four regions of the rat heart. These preliminary findings suggest that [18F]-4 could be used to assess neuronal damage in various heart diseases by positron emission tomography.
MISLANKAR, SURESH G.;GILDERSLEEVE, DAVID L.;WIELAND, DONALD M.;MASSIN, CH+, J. MED. CHEM., 31,(1988) N 2, 362-366
作者:MISLANKAR, SURESH G.、GILDERSLEEVE, DAVID L.、WIELAND, DONALD M.、MASSIN, CH+
DOI:——
日期:——
WIELAND, DONALD M.;ROSENSPIRE, KAREN C.;HUTCHINS, GARY D.;VAN, DORT MARCI+, J. MED. CHEM., 33,(1990) N, C. 956-964
作者:WIELAND, DONALD M.、ROSENSPIRE, KAREN C.、HUTCHINS, GARY D.、VAN, DORT MARCI+