Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.
[(3)H]BBL454, a new CCK(2) selective tritiated agonist was prepared via the reductive tritiation of a 5-aminopentyn-1-yl moiety introduced on the N-terminal end of a pentapeptide derivative of cholecystokinin. The binding properties of this labelled compound were determined on CHO cells transfected with the rat CCK(2) receptor. [(3)H]BBL454 is able to discriminate two affinity states of the CCK(2) receptor a supplementary indication of its validity for further exploring the heterogeneity of this receptor.
Bellier
Bruno
B
Laboratoire de Pharmacochimie Moléculaire et Structurale, FRE CNRS 2463-INSERM U266, UFR des Sciences Pharmaceutiques et Biologiques, 4 avenue de l'Observatoire, 75270 Cedex 06, Paris, France.
Dugave
Christophe
C
Etivant
Frédéric
F
Genet
Roger
R
Gigoux
Véronique
V
Garbay
Christiane
C
D000818:Animals; D016466:CHO Cells; D002766:Cholecystokinin / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000378:metabolism*; D006224:Cricetinae; D006168:Guinea Pigs; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000378:metabolism; D010446:Peptide Fragments / Q000138:chemical synthesis* / Q000378:metabolism*; D011869:Radioligand Assay / Q000379:methods; D051381:Rats; D043887:Receptor, Cholecystokinin B / Q000819:agonists* / Q000378:metabolism; D014316:Tritium / Q000378:metabolism
C490102:(3H)BBL454, peptide; D009842:Oligopeptides; D010446:Peptide Fragments; D043887:Receptor, Cholecystokinin B; D014316:Tritium; D002766:Cholecystokinin