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Pyrazolo[3,4-d]pyrimidines as Sigma-1 Receptor Ligands for the Treatment of Pain. Part 2: Introduction of Cyclic Substituents in Position 4

Abstract

The replacement of acylamino by cyclic substituents in the 4 position of the pyrazolo[3,4-d]pyrimidine scaffold, led to highly active sigma-1 receptor (σ1R) ligands. Phenyl or pyrazolyl groups were the best in terms of affinity for the σ1R and the 4-(1-methylpyrazol-5-yl) derivative, 12f, was the most selective. Compound 12f is also one of the best σ1R ligands ever described in terms of lipophilic ligand efficiency, which translates into a good physicochemical and ADMET profile. In addition, 12f was identified as an antagonist of the σ1R in view of its potent antinociceptive profile in several pain models in mice.

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Publication details

The article was received on 16 Feb 2017, accepted on 08 Apr 2017 and first published on 20 Apr 2017


Article type: Research Article
DOI: 10.1039/C7MD00078B
Citation: Med. Chem. Commun., 2017, Accepted Manuscript
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    Pyrazolo[3,4-d]pyrimidines as Sigma-1 Receptor Ligands for the Treatment of Pain. Part 2: Introduction of Cyclic Substituents in Position 4

    J. L. Díaz, J. Corbera, D. Martinez, M. Bordas, C. Sicre, R. Pascual, M. J. Pretel, A. P. Marín, A. Montero, A. Dordal, I. ALVAREZ and C. Almansa, Med. Chem. Commun., 2017, Accepted Manuscript , DOI: 10.1039/C7MD00078B

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