Synthesis and biochemical properties of an 125I-labelled ryanodine derivative.
The synthesis of a novel radioiodinated ryanodine-O10eq-N-acylamino acylate along with biological data are reported. The affinity of the iodinated product, 7, was comparable to ryanodine, 7.97 nM and 6.47 nM, respectively. Conversion of the non-radioactive iodinated ryanodine analog to the [125I] isotope was accomplished by conversion of 7 to the trimethyltin derivative followed by [125I] exchange using chloramine-T in organic solvent. The radioiodinated ryanodine analog, 9, bound to cardiac membrane preparations in a protein dependent and saturable manner indicating that this analog may represent a useful new tool for the study of ryanodine receptors and that modifications about the C-10 hydroxy group of ryanodine may be carried out without loss in biological activity.
Mais
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Cardiovascular Department Eli Lilly and Company, Indianapolis, Indiana 46285.
Bowling
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Watanabe
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D000818:Animals; D002118:Calcium / Q000378:metabolism*; D004285:Dogs; D007457:Iodine Radioisotopes; D008566:Membranes / Q000378:metabolism; D009124:Muscle Proteins / Q000378:metabolism*; D009206:Myocardium / Q000378:metabolism*; D011950:Receptors, Cholinergic / Q000378:metabolism*; D012433:Ryanodine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D019837:Ryanodine Receptor Calcium Release Channel
D007457:Iodine Radioisotopes; D009124:Muscle Proteins; D011950:Receptors, Cholinergic; D019837:Ryanodine Receptor Calcium Release Channel; D012433:Ryanodine; D002118:Calcium