The synthesis of the αvβ3 integrin receptor ligand [125I]L-775,219.

被引:10
作者
Hamill, TG
Duggan, ME
Perkins, JJ
机构
[1] Merck Res Labs, Dept Pharmacol, West Point, PA 19486 USA
[2] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA
关键词
iodine-125; vitronectin; alpha(V)beta(3) integrin; radioiodination;
D O I
10.1002/jlcr.432
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The alpha (v)beta (3) integrin receptor ligand [I-125]L-775,219, 1c, was synthesized for use in an in vitro receptor binding assay with high specific activity (>1500 Ci/mmol) and a radiochemical yield of 15-20%. Conversion of iodide 1b to the corresponding aryl trimethylstannane 2, followed by radioiodination using (NaI)-I-125/iodobead gave 1c.
引用
收藏
页码:55 / 59
页数:5
相关论文
共 8 条
[1]  
CHAMBERS TJ, 1986, BONE MINER, V1, P127
[2]   Antibody to beta(3) integrin inhibits osteoclast-mediated bone resorption in the thyroparathyroidectomized rat [J].
Crippes, BA ;
Engleman, VW ;
Settle, SL ;
Delarco, J ;
Ornberg, RL ;
Helfrich, MH ;
Horton, MA ;
Nickols, GA .
ENDOCRINOLOGY, 1996, 137 (03) :918-924
[3]  
DUGGAN ME, IN PRESS J MED CHEM
[4]   A peptidomimetic antagonist of the alpha(v)beta(3) integrin inhibits bone resorption in vitro and prevents osteoporosis in vivo [J].
Engelman, VW ;
Nickols, GA ;
Ross, FP ;
Horton, MA ;
Griggs, DW ;
Settle, SL ;
Ruminski, PG ;
Teitelbaum, SL .
JOURNAL OF CLINICAL INVESTIGATION, 1997, 99 (09) :2284-2292
[5]  
Lark MW, 1999, J PHARMACOL EXP THER, V291, P612
[6]   Recent advances in cell adhesion molecules and extracellular matrix proteins: Potential clinical implications [J].
Mousa, SA ;
Cheresh, DA .
DRUG DISCOVERY TODAY, 1997, 2 (05) :187-199
[7]  
Rodan SB, 1997, J ENDOCRINOL, V154, pS47
[8]   The integrin ligand echistatin prevents bone loss in ovariectomized mice and rats [J].
Yamamoto, M ;
Fisher, JE ;
Gentile, M ;
Seedor, JG ;
Leu, CT ;
Rodan, SB ;
Rodan, GA .
ENDOCRINOLOGY, 1998, 139 (03) :1411-1419