Roflumilast inhibits the release of chemokines and TNF‐α from human lung macrophages stimulated with lipopolysaccharide

No abstract is available for this paper.

• Publication year

  2012

• Venue

  British Journal of Pharmacology

• Publication date

  2012-03-01

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1111/j.1476-5381.2011.01667.xPMID 21913898PMCID PMC3372837
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Guide to Receptors and Channels (GRAC), 5th edition

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  2010influential reference
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  2010influential reference
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  2010influential reference
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  2008influential reference
• Guide to Receptors and Channels (GRAC), 3rd edition

  2008cited by this paper
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  2001influential reference
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  1999influential reference
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  1997influential reference
• Beta 2-adrenergic activation enhances interleukin-8 production by human monocytes.

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  1996cited by this paper
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  1995influential reference
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  1994cited by this paper
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