Synthesis and biochemical properties of an 125I-labelled ryanodine derivative

Biochem Biophys Res Commun. 1992 Mar 16;183(2):462-7. doi: 10.1016/0006-291x(92)90504-e.

Abstract

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.

MeSH terms

  • Animals
  • Calcium / metabolism*
  • Dogs
  • Iodine Radioisotopes
  • Membranes / metabolism
  • Muscle Proteins / metabolism*
  • Myocardium / metabolism*
  • Receptors, Cholinergic / metabolism*
  • Ryanodine / analogs & derivatives*
  • Ryanodine / chemistry
  • Ryanodine / metabolism
  • Ryanodine Receptor Calcium Release Channel

Substances

  • Iodine Radioisotopes
  • Muscle Proteins
  • Receptors, Cholinergic
  • Ryanodine Receptor Calcium Release Channel
  • Ryanodine
  • Calcium