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Updated: Jul 19, 2026

Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
Published on: May 24, 2024
Neuropeptide and kinin antagonists
1Merck, Sharp and Dohme Research Laboratories, Terlings Park, Harlow, Essex CM20 2QR, UK. hillr@merck.com
Abstract:
Neuropeptides and kinins are important messengers in the nervous system and--on the basis of their anatomical localisation and the effects produced when the substances themselves are administered, to animals or to human subjects-a significant number of them have been suggested to have a role in pain and inflammation. Experiments in gene deletion (knock-out or null mutant) mice and parallel experiments with pharmacological receptor antagonists in a variety of species have strengthened the evidence that a number of peptides, notably substance P and calcitonin gene-related peptide (CGRP), and the kinins have a pathophysiological role in nociception. Clinical studies with non-peptide pharmacological antagonists are now in progress to determine if blocking the action of these peptides might have utility in the treatment of pain.
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