69994-38-3Relevant academic research and scientific papers
Tritiated Peptides. Part 15. Synthesis of Tritium Labelled Biologically Active Analogues of Somatostatin
Allen, Mark C.,Brundish, Derek E.,Fullerton, Joseph D.,Wade, Roy
, p. 989 - 1004 (2007/10/02)
The syntheses are described of cyclo-8,Gaba12>somatostatin-(5-12)-peptide> (77), and (79)-(82) labelled singly at positions 6, 7, 8, and 11 and doubly at residues 6 and 11 to specific radioactivities of between 4.8 and 22.4 Ci mmol-1.The linear sequence (5-12) and the related cyclo8,Nag12>somatostatin-(5-12)-peptide> (78) and (83) were also prepared to specific radioactivities of 19.2 and 19.6 Ci mmol-1 respectively.The syntheses of the labelled hexapeptide cyclo-7,D-Trp8,Pro12>somatostatin-(7-12)-peptide> (84) and full sequences 6,D-Trp8,D-Cys14>somatostatin (94) and 8,4-(3)H-Phe11,D-Cys14>somatostatin (95) labelled at ca. 13.0 Ci mmol-1 are described.Labelling was effected by reductive dehalogenation in the presence of tritium of the fully protected precursors and the purity of the final products was assessed by amino acid analysis after acidic hydrolysis following purification by ion-exchange and h.p.l.c. as appropriate.
Tritiated Peptides. Part 11. Synthesis of 6>-, 11>-, and 6,11>-Somatostatin and the Metabolite 1>-Somatostatin
Allen, Mark C.,Brundish, Derek E.,Martin, John R.,Wade, Roy
, p. 2040 - 2048 (2007/10/02)
The syntheses are described of somatostatin labelled with tritium singly in the phenylalanine residues at positions 6 and 11 and doubly at residues 6 and 11 to specific radioactivities of 15.5, 13.8 and 14.1 Cim mol-1, respectively, by reductive deiodination of fully-protected precursors.Cysteine residues were proteced by S-trityl groups and the disulphide bridge was formed by iodine oxidation of the tritiated protected precursors.The purity of the products was assessed by acidic hydrolysis, ion-exchange and high-pressure liquid chromatography, and by enzymic digestion of the products modified by reduction and aminoethylation.The synthesis of the metabolite 1>-somatostatin is described.The syntheses of 6>-, 11>- and 6,11>-somatostatin are described.
