Simultaneous tritium labelling of two potent 5-HT4 ligands.
Two potent and selective 5-HT(4) ligands, [(3)H]-5-[(N-propylpiperidin-4-yl)methoxy]-1,2,3,4-tetrahydrobenzo[h][1,6] naphthyridine (1a) and [(3)H]-1-methyl-5-[(N-propylpiperidin-4-yl)methoxy]pyrrolo[1,2-a]thieno[2,3-e]pyrazine (2a) were radiolabelled with tritium. Radioactive labelling was achieved by simultaneous tritium reduction of a mixture of both propargylic precursors (1c-2c). The two tritiated ligands thus obtained were radiochemically pure and possessed high radioactive specific activities. These tritiated 5-HT(4) ligands will allow for binding characterization as an essential tool for their further development.
Sobrio
Franck
F
CEA, I(2)BM, CI-NAPS, LDM-TEP, Université de Caen Basse-Normandie, UMR 6232 CI-NAPS, F-14074 Caen, France. sobrio@cyceron.fr
Lemaitre
Stéphane
S
Hinsberger
Antoine
A
Barré
Louisa
L
Rousseau
Bernard
B
Rault
Sylvain
S
D008024:Ligands; D015394:Molecular Structure; D009287:Naphthyridines / Q000737:chemistry*; D010880:Piperidines / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000737:chemistry*; D058825:Serotonin 5-HT1 Receptor Agonists
C550282:((3)H)-1-methyl-5-((N-propylpiperidin-4-yl)methoxy)pyrrolo(1,2-a)thieno(2,3-e)pyrazinenzo(h)(1,6)naphthyridine; C550203:((3)H)-5-((N-propylpiperidin-4-yl)methoxy)-1,2,3,4-tetrahydrobenzo(h)(1,6) naphthyridine; D008024:Ligands; D009287:Naphthyridines; D010880:Piperidines; D019275:Radiopharmaceuticals; D058825:Serotonin 5-HT1 Receptor Agonists