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Pharmacodynamics is a scientific field that delves into drugs' intricate biochemical, cellular, and physiological effects on the human body. The study of pharmacodynamics helps us understand how drugs interact with the body and elicit various responses.
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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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Updated: Jul 7, 2025

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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The Concise Guide to PHARMACOLOGY 2023/24: Catalytic receptors.

Stephen P H Alexander1, Doriano Fabbro2, Eamonn Kelly3

  • 1School of Life Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK.

British Journal of Pharmacology
|December 20, 2023
PubMed
Summary
This summary is machine-generated.

The Concise Guide to Pharmacology 2023/24 offers a comprehensive overview of drug targets and their interactions. This biennial publication provides essential pharmacology data for researchers and clinicians.

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Area of Science:

  • Pharmacology
  • Drug Discovery
  • Biomedical Research

Background:

  • The Concise Guide to Pharmacology is a biennial publication series.
  • It summarizes key properties of drug targets and their interactions.
  • The guide links to an open-access knowledgebase for detailed information.

Purpose of the Study:

  • To provide a concise, citable, point-in-time record of pharmacological data.
  • To offer an overview of approximately 1800 drug targets and 6000 ligand interactions.
  • To present official IUPHAR classification and nomenclature for human drug targets.

Main Methods:

  • Data compilation in a tabular format.
  • Inclusion of selective pharmacology where available.
  • Cross-referencing with the online guide (https://www.guidetopharmacology.org/).

Main Results:

  • Overview of ~1800 drug targets and ~6000 ligand interactions.
  • Categorization of targets into six major groups: catalytic receptors, G protein-coupled receptors, ion channels, nuclear hormone receptors, enzymes, and transporters.
  • Inclusion of nomenclature guidance and information on pharmacological tools.

Conclusions:

  • The Concise Guide serves as a permanent, citable record of pharmacology data.
  • It facilitates comparison of related targets.
  • The publication provides essential resources for researchers in pharmacology and drug discovery.