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Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
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When a drug follows nonlinear pharmacokinetics, its bioavailability, the amount of the drug that reaches the systemic circulation, can change with different doses. This is due to the presence of a saturable pathway. The pathway becomes saturated as the drug concentration increases, decreasing the absorption rate. Consequently, the drug's bioavailability may be lower than expected at higher doses.
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Principles of Drug Action01:24

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The Concise Guide to PHARMACOLOGY 2025/26: Introduction and Other Protein Targets.

Stephen P H Alexander1, Alasdair J Gibb2, Eamonn Kelly3

  • 1Division of Physiology, Pharmacology & Neuroscience, School of Life Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK.

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This summary is machine-generated.

The Concise Guide to Pharmacology 2025/26 offers a comprehensive yet accessible overview of human drug targets and their interactions. This biennial publication provides expert-curated pharmacological tools and nomenclature for drug discovery.

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Area of Science:

  • Pharmacology
  • Drug Discovery
  • Biochemistry

Background:

  • The British Journal of Pharmacology publishes biennial updates to the Concise Guide to Pharmacology.
  • The guide provides a comparative overview of drug target families.
  • The 2025/26 edition is the seventh in this series.

Purpose of the Study:

  • To provide a clear, accessible, and well-structured summary of human drug targets and their interactions.
  • To offer expert-curated recommendations of selective pharmacological tools for target identification.
  • To serve as a permanent, citable, point-in-time record of pharmacological information.

Main Methods:

  • Summarization of key pharmacological properties for approximately 1900 human drug targets.
  • Inclusion of nearly 7000 interactions involving around 4400 ligands.
  • Focus on six key areas: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors, enzymes, and transporters.

Main Results:

  • The guide details the pharmacology of approximately 1900 human drug targets and 7000 interactions.
  • It provides official IUPHAR (International Union of Basic and Clinical Pharmacology) classification and nomenclature where applicable.
  • Expert-curated recommendations for 'Gold Standard' selective pharmacological tools are included.

Conclusions:

  • The Concise Guide to Pharmacology 2025/26 serves as a valuable, stable reference for researchers.
  • It complements the online Guide to Pharmacology website by providing a citable snapshot of current knowledge.
  • The guide facilitates drug discovery by offering curated information on drug targets and pharmacological tools.