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A non-peptide radioiodinated high affinity melanocortin-4 receptor ligand

✍ Scribed by Felikss Mutulis; Sviatlana Yahorava; Ilze Mutule; Aleh Yahorau; Sergei Kopanchuk; Santa Veiksina; Ago Rinken; Jarl E. S. Wikberg

Book ID
102374085
Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
146 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

4‐Cyclohexyl‐4‐[(1,2,4‐triazol‐1‐yl)methyl]piperidine was introduced into stepwise peptide synthesis procedures using Boc chemistry and derivatives of D‐4‐iodophenylalanine and D‐1,2,3,4‐tetrahydroisoquinoline‐3‐carboxylic acid. A halogen replacement analogue (I‐Mex2) of a known high affinity melanocortin‐4 receptor selective compound resulted. It showed a subnanomolar affinity when evaluated on the melanocortin‐4 receptor in competition with the α‐MSH peptide analogue ^125^I‐NDP‐MSH. By treatment with hexamethylditin and tetrakis(triphenylphosphine) palladium I‐Mex2 was converted to the corresponding trimethylstannyl derivative. In the next step, Na^125^I was oxidized by an iodobead. Iododestannylation proceeded in the presence of 1 M phosphate buffer, pH 2.5, and the radio‐active derivative ^125^I‐Mex2 formed was separated by HPLC at 40% radiochemical yield. Preliminary investigation showed that ^125^I‐Mex2 is useful as a radioligand for melanocortin‐4 receptor binding studies. Copyright © 2003 John Wiley & Sons, Ltd.

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