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Open Access

Novel pyrazole inhibitors for discrimination between receptor-operated and store-operated Ca2+ entry

  • Hannes Schleifer1,
  • Regina Oppenrieder1,
  • Sonia Stürmer1,
  • Bernhard Doleschal1,
  • Michael Poteser1,
  • Toma N Glasnov2,
  • C Oliver Kappe2 and
  • Klaus Groschner1Email author
BMC Pharmacology201111(Suppl 2):A18

https://doi.org/10.1186/1471-2210-11-S2-A18

Published: 5 September 2011

Background

Calcium governs a wide range of cellular processes. Specifically, control of gene transcription involves Ca2+ entry channels that are activated by either voltage, second messengers or depletion of intracellular stores. The family of classical transient receptor potential channels (TRPC) has been implicated in both the receptor/second messenger as well as in store-operated Ca2+ entry pathway, and represents an attractive target for therapeutic intervention.

Methods

We tested a series of pyrazol compound structurally related to Pyr3 [1], a recently discovered TRPC3 inhibitor, for effects on receptor- as well as store-operated Ca2+ entry into RBL-2H3 mast cells and HEK293 cells overexpressing TRPC3.

Results and conclusions

We identified novel Ca2+ entry inhibitors, which are able to discriminate between the two tightly related pathways of receptor/second messenger-activated and store-operated calcium entry. These compounds appear suitable for selective modulation of Ca2+-dependent gene transcription in a variety of mammalian cells.

Declarations

Acknowledgements

Supported by the Austrian Science Fund FWF project P21925-B19 and P21118-B09.

Authors’ Affiliations

(1)
Institute for Pharmaceutical Sciences, Pharmacology & Toxicology, University of Graz
(2)
Institute of Chemistry, Christian Doppler Laboratory for Microwave Chemistry University of Graz

References

  1. Glasnov TN, Groschner K, Kappe CO: High-speed microwave-assisted synthesis of the trifluoromethylpyrazol-derived canonical transient receptor potential (TRPC) channel inhibitor Pyr3. ChemMedChem. 2009, 4: 1816-1818. 10.1002/cmdc.200900304.View ArticlePubMedGoogle Scholar

Copyright

© Schleifer et al; licensee BioMed Central Ltd. 2011

This article is published under license to BioMed Central Ltd. This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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