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.

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http://dx.doi.org/10.1016/j.bmcl.2005.11.037DOI Listing

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