title: Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors.
abstract: The synthesis and the preliminary biological evaluation of the first high affinity radioligand antagonist for the human A3 adenosine receptor, named [3H]-MRE 3008-F20 are reported. [3H]-MRE 3008-20 bound human A3 receptors expressed in CHO cells with K(D) and Bmax value of 0.82 +/- 0.08 nM and 297 +/- 28 fmol/mg of protein, respectively. [3H]-MRE 3008-F20 represents a useful tool for a further characterization of A3 adenosine receptor subtype.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy. pgb@dns.unife.it
authors.forename: P G
authors.initials: PG
authors.lastname: Baraldi
authors.forename: B
authors.initials: B
authors.lastname: Cacciari
authors.forename: R
authors.initials: R
authors.lastname: Romagnoli
authors.forename: K
authors.initials: K
authors.lastname: Varani
authors.forename: S
authors.initials: S
authors.lastname: Merighi
authors.forename: S
authors.initials: S
authors.lastname: Gessi
authors.forename: P A
authors.initials: PA
authors.lastname: Borea
authors.forename: E
authors.initials: E
authors.lastname: Leung
authors.forename: S L
authors.initials: SL
authors.lastname: Hickey
authors.forename: G
authors.initials: G
authors.lastname: Spalluto
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D010671:Phenylurea Compounds / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D058915:Purinergic P1 Receptor Antagonists; D011869:Radioligand Assay; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1 / Q000378:metabolism; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D014230:Triazoles / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D014316:Tritium
chemical_list: C405605:MRE 3008-F20; D010671:Phenylurea Compounds; D058915:Purinergic P1 Receptor Antagonists; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1; D011994:Recombinant Proteins; D014230:Triazoles; D014316:Tritium