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.
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.
Baraldi
Pier Giovanni
PG
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, 44100 Ferrara, Italy. baraldi@unife.it
Pavani
Maria Giovanna
MG
Leung
Edward
E
Moorman
Allan R
AR
Varani
Katia
K
Vincenzi
Fabrizio
F
Borea
Pier Andrea
PA
Romagnoli
Romeo
R
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
C508856:(2-amino-4,5,6,7-tetrahydrobenzo(b)thiophen-3-yl)-(4-chlorophenyl)methanone; D043682:Receptor, Adenosine A1; D013876:Thiophenes; D014316:Tritium