title: Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.
abstract: [(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.
authors.affiliation: 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.
authors.forename: Bruno
authors.initials: B
authors.lastname: Bellier
authors.forename: Christophe
authors.initials: C
authors.lastname: Dugave
authors.forename: Frédéric
authors.initials: F
authors.lastname: Etivant
authors.forename: Roger
authors.initials: R
authors.lastname: Genet
authors.forename: Véronique
authors.initials: V
authors.lastname: Gigoux
authors.forename: Christiane
authors.initials: C
authors.lastname: Garbay
mesh_terms: 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
chemical_list: C490102:(3H)BBL454, peptide; D009842:Oligopeptides; D010446:Peptide Fragments; D043887:Receptor, Cholecystokinin B; D014316:Tritium; D002766:Cholecystokinin