title: Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer.
abstract: Among the adenosine A(1) allosteric enhancers reported so far, compound (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone 1 (named T-62) has shown biological properties similar to those of PD 81,723, the reference A(1) allosteric enhancer and it has been more fully pharmacologically investigated. The preparation of the radiolabelled form of compound 1 and its characterization by saturation binding experiments are reported. These studies allowed us to demonstrate for the first time the existence of a specific, allosteric site on the A(1) receptor.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Ferrara, 44100 Ferrara, Italy. baraldi@unife.it
authors.forename: Pier Giovanni
authors.initials: PG
authors.lastname: Baraldi
authors.forename: Maria Giovanna
authors.initials: MG
authors.lastname: Pavani
authors.forename: Edward
authors.initials: E
authors.lastname: Leung
authors.forename: Allan R
authors.initials: AR
authors.lastname: Moorman
authors.forename: Katia
authors.initials: K
authors.lastname: Varani
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Vincenzi
authors.forename: Pier Andrea
authors.initials: PA
authors.lastname: Borea
authors.forename: Romeo
authors.initials: R
authors.lastname: Romagnoli
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D015394:Molecular Structure; D043682:Receptor, Adenosine A1 / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014316:Tritium
chemical_list: C508856:(2-amino-4,5,6,7-tetrahydrobenzo(b)thiophen-3-yl)-(4-chlorophenyl)methanone; D043682:Receptor, Adenosine A1; D013876:Thiophenes; D014316:Tritium