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Tritium labelling and degradation studies of Dmt 1 ‐endomorphin 2
Author(s) -
Szemenyei Erzsébet,
Tóth Géza
Publication year - 2007
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1402
Subject(s) - chemistry , tritium , hydrolysis , nuclear chemistry , degradation (telecommunications) , labelling , chromatography , radiochemistry , medicinal chemistry , organic chemistry , biochemistry , telecommunications , physics , computer science , nuclear physics
Two tritiated derivatives of Dmt 1 ‐endomorphin 2 (Dmt 1 ‐EM2) were prepared by the catalytic tritiodehalogenation of 3′,5′‐diiodo‐Dmt 1 ‐EM2 and the saturation of 3,4 ΔPro 2 ‐Dmt 1 ‐EM2, resulting in [3′,5′‐ 3 H 2 ]Dmt 1 ‐EM2 and [ 3 H 2 ]Pro 2 ‐Dmt 1 ‐EM2 with specific activities of 2.88 TBq/mmol (77.8 Ci/mmol) and 1.95 TBq/mmol (52.8 Ci/mmol), respectively. 3′,5′‐Diiodo‐Dmt 1 ‐EM2 was synthesized by the chloramine T method from Dmt 1 ‐EM2. 3,4 ΔPro 2 ‐Dmt 1 ‐EM2 was synthesized by using the Merrifield solid‐phase method. The distributions of the tritium in the labelled peptides were investigated by reversed‐phase high‐performance liquid chromatography after acidic hydrolysis. The stability of Dmt 1 ‐EM2 in a rat brain membrane homogenate was also determined. Copyright © 2007 John Wiley & Sons, Ltd.