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Updated: Oct 3, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Agonists of proteinase-activated receptor 2 excite guinea pig ileal myenteric neurons
D R Linden1, B P Manning, N W Bunnett
1Given C 423, Department of Anatomy and Neurobiology, The University of Vermont College of Medicine, Burlington, VT 05405, USA.
Abstract:
The effects of proteinase-activated receptor 2 (PAR2) agonists on the electrical properties of intact guinea pig ileal myenteric neurons were measured with intracellular microelectrodes. Approximately 52% of AH neurons and 41% of S neurons responded to pressure ejection of SLIGRL-NH(2) or trypsin with a prolonged depolarization that was often accompanied by increased excitability. When added to the bathing solution, trypsin caused a concentration-dependent depolarization of responding neurons with an estimated EC(50) value of 87 nM. Collectively, these novel observations indicate that PAR2 excites a proportion of myenteric neurons, which may contribute to dysmotility during intestinal inflammation.
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