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Bioorg Med Chem Lett. 2006 Mar 1;16(5):1402-4.

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.

Author information

1
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, 44100 Ferrara, Italy. baraldi@unife.it

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.

PMID:
16321527
DOI:
10.1016/j.bmcl.2005.11.037
[Indexed for MEDLINE]

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