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

doi:10.1016/0006-291X(92)90504-E

Biochemical and Biophysical Research Communications

Volume 183, Issue 2, 16 March 1992, Pages 462-467

https://doi.org/10.1016/0006-291X(92)90504-E Get rights and content

Abstract

The synthesis of a novel radioiodinated ryanodine-O_10eq-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.

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

Abstract

J. Am. Chem. Soc

Adv. Org. Chem

J. Chem. Soc. Chem. Commun

J. Chem. Soc. Perkin Trans

Pharmacol. Rev

J. Gen. Physiol

J. Biol. Chem

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