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Tritium labelling and degradation studies of Dmt1-endomorphin 2

✍ Scribed by Erzsébet Szemenyei; Géza Tóth

Publisher
John Wiley and Sons
Year
2007
Tongue
French
Weight
102 KB
Volume
50
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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.

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