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Synthesis and tritium labeling of the highly potent mast cell‐degranulating substance P analog H‐Arg‐Pro‐Lys‐Pro‐NH‐C 12 H 25
Author(s) -
Bienert M.,
Oehlke J.,
Mittag E.,
Niedrich H.
Publication year - 1990
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.2580281207
Subject(s) - chemistry , triethylamine , dimethylformamide , catalysis , tritium , nuclear chemistry , mast cell , medicinal chemistry , stereochemistry , organic chemistry , physics , solvent , nuclear physics , immunology , biology
Tritium labeling of the mast cell degranulating substance P analog H‐Arg‐Pro‐Lys(3,4‐ 3 H‐Pro)‐NH‐C 12 H 25 by catalytic saturation of the dehydroproline (Dhp Abbreviations: Ac, acetyl; Dhp, L‐3,4‐dehydroproline; DMA, dimethyl‐acetamide; DMF, dimethylformamide; HOBt, 1‐hydroxybenzotriazole; MA, mixed anhydride coupling; NMM, N‐methylmorpholine; ONSu, N‐hydroxysuccinimide ester; TEA, triethylamine. ) double bond is described. Catalytic tritiation in water afforded the radioactive analog with a specific activity of 1.07 TBq/mmol. Tenfold enhancement of the catalyst‐to‐substrate ratio resulted in a reduced specific activity of 0.74 TBq/mmol.