PD 102807

PD 102807 is an antagonist of the M₄ muscarinic acetylcholine receptor (mAChR) and a biased ligand of the M₃ mAChR.^1,2 It selectively binds to the M₄ receptor (IC₅₀ = 0.09 µM) over the M₁, M₂, M₃, and M₅ receptors (IC₅₀s = 6.56, 3.44, 0.95, and 7.41 µM, respectively).¹ PD 102807 inhibits carbachol-induced inhibition of forskolin-stimulated cAMP production in CHO cells expressing the M₄ or M₂ receptor (IC₅₀s = 0.4 and 3.8 nM, respectively) and, to a lesser extent, inhibits carbachol-induced phosphatidylinositol (PI) hydrolysis in CHO cells expressing the M₁, M₃, or M₅ receptors (IC₅₀s = 10, 0.88, and 25.2 µM, respectively). It induces β-arrestin recruitment but inhibits methacholine-induced calcium mobilization in HEK293 cells expressing the M₃ receptor at 100 µM.² PD 102807 (10 µM) reduces TGF-β-induced hypercontractility in human airway smooth muscle cells.

WARNING This product is not for human or veterinary use.

1. Augelli-Szafran, C.E., Jaen, J.C., Moreland, D.W., et al. Identification and characterization of m4 selective muscarinic antagonists. Biooorg. Med. Chem. Lett. 8(15), 1991-1996 (1998).

2. Tompkins, E., Mimic, B., Cuevas-Mora, K., et al. PD 102807 induces M3 mAChR-dependent GRK-/arrestin-biased signaling in airway smooth muscle cells. Am. J. Respir. Cell Mol. Biol. 67(55), 550-561 (2022).