Crofelemer, an Antisecretory Antidiarrheal Proanthocyanidin Oligomer Extracted from Croton lechleri, Targets Two Distinct Intestinal Chloride Channels

No abstract is available for this paper.

• Publication year

  2010

• Venue

  Molecular Pharmacology

• Publication date

  2010-01-01

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1124/mol.109.061051PMID 19808995PMCID PMC2802429
• 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.

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  2009influential reference
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  1993cited by this paper
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  1992influential reference

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