✦ LIBER ✦
Synthesis of S-[3-(4(5)-imidazolyl)propyl],N-[2(4-{125I}-iodophenyl)ethyl]isothiourea sulfate (125I-iodophenpropit), a new probe for histamine H3 receptor binding sites.
✍ Scribed by Wiro M. P. B. Menge; Henk Van Der Goot; Hendrik Timmerman; Jos. L. H. Eersels; Jacobu S. D. M. Herscheid
- Publisher
- John Wiley and Sons
- Year
- 1992
- Tongue
- French
- Weight
- 327 KB
- Volume
- 31
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
The synthesis of the first high specific activity {^125^I} labelled selective H~3~ antagonist, Iodophenpropit‐ i.e., S‐[3‐(4(5)‐imidazolyl)propyl],N‐[2‐(4‐{^125^I}‐iodophenyl)ethyl]isothiourea sulfate is reported.
The radiolabelled compound was prepared by Cu(I)assisted nucleophilic non‐isotopic exchange from the corresponding bromo derivative (VUF 4598). The ^125^I‐Iodophenpropit was purified using reverse phase HPLC and obtained in a chemical and radiochemical purity >98% and a specific activity of 1900 Ci/mmol.