Synthesis of S‐[3‐(4(5)‐imidazolyl)propyl],N‐[2(4‐{ 125 I}‐iodophenyl)ethyl]isothiourea sulfate ( 125 I‐iodophenpropit), a new probe for histamine H 3 receptor binding sites.
1992; Wiley; Volume: 31; Issue: 10 Linguagem: Inglês
10.1002/jlcr.2580311007
ISSN1099-1344
AutoresWiro M. P. B. Menge, H. van der Goot, H. Timmerman, Jos Eersels, Jacobu S. D. M. Herscheid,
Tópico(s)Polyamine Metabolism and Applications
ResumoAbstract 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.
Referência(s)