ALPHA-METHYLENE AND GLYCIDIC ACID ANALOGS OF IPPA AS POTENTIAL MYOCARDIAL IMAGING AGENTS

被引:0
作者
RUYAN, MK
BAKAN, DA
SKINNER, RWS
NEWMAN, C
GROSS, MD
COUNSELL, RE
机构
[1] UNIV MICHIGAN,SCH MED,DEPT PHARMACOL,ANN ARBOR,MI 48109
[2] UNIV MICHIGAN,SCH MED,DEPT MED CHEM,ANN ARBOR,MI 48109
[3] VET ADM MED CTR,DEPT VET AFFAIRS,NUCL MED SERV,ANN ARBOR,MI 48104
来源
NUCLEAR MEDICINE AND BIOLOGY | 1995年 / 22卷 / 01期
关键词
D O I
10.1016/0969-8051(94)E0067-S
中图分类号
R8 [特种医学]; R445 [影像诊断学];
学科分类号
1002 ; 100207 ; 1009 ;
摘要
Using organozinc cross-coupling reactions, two radiolabeled analogs of 15-(p-iodophenyl) pentadecanoic acid (IPPA) have been designed and synthesized as potential scintigraphic imaging agents for the heart. Both 15-(4-iodophenyl)-tridecylglycidic acid and 15-(4-iodophenyl)-2-methylene pentadecanoic acid were synthesized and radioiodinated. In tissue biodistribution studies in rats, only the alpha-methylene derivative of IPPA displayed a consistently higher heart to blood ratio and a substantially lower degree of thyroid accumulation than did IPPA alone. With respect to a scintigraphic imaging efficacy, the alpha-methylene analog of IPPA and IPPA itself showed essentially equivalent cardiac imaging profiles in rabbits, with a slight extension in imaging time for the alpha-methylene analog of IPPA.
引用
收藏
页码:95 / 103
页数:9
相关论文
共 22 条
[1]   SYNTHESIS OF FATTY-ACIDS USING ORGANOCOPPER(I) ATE COMPLEXES DERIVED FROM GRIGNARD-REAGENTS [J].
BERGBREITER, DE ;
WHITESIDES, GM .
JOURNAL OF ORGANIC CHEMISTRY, 1975, 40 (06) :779-782
[2]  
Chilton HM, 1990, PHARM MED IMAGING, P419
[3]  
DEGRADO TR, 1991, J NUCL MED, V32, P1888
[4]  
FREUNDLIEB C, 1980, J NUCL MED, V21, P1043
[5]  
GOODMAN MM, 1982, J NUCL MED, V23, P904
[6]   SYNTHESIS AND EVALUATION OF RADIOIODINATED TERMINAL PARA-IODOPHENYL-SUBSTITUTED ALPHA-METHYL-BRANCHED AND BETA-METHYL-BRANCHED FATTY-ACIDS [J].
GOODMAN, MM ;
KIRSCH, G ;
KNAPP, FF .
JOURNAL OF MEDICINAL CHEMISTRY, 1984, 27 (03) :390-397
[7]  
GOODMAN MM, 1983, J NUCL MED, V23, P904
[8]  
KIORPES TC, 1984, J BIOL CHEM, V259, P9750
[9]  
KNAPP FF, 1986, J NUCL MED, V27, P521
[10]   NUCLEOPHILIC REACTIVITY OF ZINC AND COPPER CARBENOIDS .2. [J].
KNOCHEL, P ;
CHOU, TS ;
CHEN, HG ;
YEH, MCP ;
ROZEMA, MJ .
JOURNAL OF ORGANIC CHEMISTRY, 1989, 54 (22) :5202-5204