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

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Abstract

Among the adenosine A1 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 A1 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 A1 receptor.

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Acknowledgment

We thank King Pharmaceuticals Research and Development for proposal and financial support.

References and notes (19)

  • P.G. Baraldi et al.

    Bioorg. Med. Chem. Lett.

    (2000)
  • P.J. Munson et al.

    Anal. Biochem.

    (1980)
  • Y.W. Lee et al.

    J. Pharmacol. Exp. Ther.

    (1996)
  • A. Christopoulos

    Nat. Rev. Drug Discov.

    (2002)
  • R.F. Bruns et al.

    Mol. Pharmacol.

    (1990)
  • R.F. Bruns et al.

    Mol. Pharmacol.

    (1990)
  • P.A.M. Van der Klein et al.

    J. Med. Chem.

    (1999)
  • S.R. Childers et al.

    J. Neurochem.

    (2005)
  • Baraldi, P. G. US Patent 5,939,432,...
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