title: 7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors.
abstract: New fluorescent ligands for adenosine receptors (ARs), obtained by the insertion, in the N(6) position of NECA, of NBD-moieties with linear alkyl spacers of increasing length, proved to possess a high affinity and selectivity for the A(3) subtype expressed in CHO cells. In fluorescence microscopy assays, compound 2d, the most active and selective for human A(3)-AR, permitted visualization and localization of this human receptor subtype, showing its potential suitability for internalization and trafficking studies in living cells.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Pisa, via Bonanno 6, 56126 Pisa, Italy. mmacchia@farm.unipi.it
authors.forename: M
authors.initials: M
authors.lastname: Macchia
authors.forename: F
authors.initials: F
authors.lastname: Salvetti
authors.forename: S
authors.initials: S
authors.lastname: Bertini
authors.forename: V
authors.initials: V
authors.lastname: Di Bussolo
authors.forename: L
authors.initials: L
authors.lastname: Gattuso
authors.forename: M
authors.initials: M
authors.lastname: Gesi
authors.forename: M
authors.initials: M
authors.lastname: Hamdan
authors.forename: K N
authors.initials: KN
authors.lastname: Klotz
authors.forename: T
authors.initials: T
authors.lastname: Laragione
authors.forename: A
authors.initials: A
authors.lastname: Lucacchini
authors.forename: F
authors.initials: F
authors.lastname: Minutolo
authors.forename: S
authors.initials: S
authors.lastname: Nencetti
authors.forename: C
authors.initials: C
authors.lastname: Papi
authors.forename: D
authors.initials: D
authors.lastname: Tuscano
authors.forename: C
authors.initials: C
authors.lastname: Martini
mesh_terms: D019830:Adenosine-5'-(N-ethylcarboxamide) / Q000737:chemistry*; D000818:Animals; D001572:Benzofurans / Q000737:chemistry; D016466:CHO Cells; D002462:Cell Membrane / Q000378:metabolism; D002478:Cells, Cultured; D006224:Cricetinae; D005456:Fluorescent Dyes / Q000737:chemistry* / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D008856:Microscopy, Fluorescence; D009574:Nitro Compounds / Q000737:chemistry; D043705:Receptor, Adenosine A2A; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1 / Q000235:genetics / Q000378:metabolism*; D011994:Recombinant Proteins / Q000235:genetics / Q000378:metabolism
chemical_list: D001572:Benzofurans; D005456:Fluorescent Dyes; D008024:Ligands; D009574:Nitro Compounds; D043705:Receptor, Adenosine A2A; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1; D011994:Recombinant Proteins; D019830:Adenosine-5'-(N-ethylcarboxamide)