PSB-KD107

PSB-KD107 is an agonist of the orphan G protein-coupled receptor GPR18 (EC₅₀ = 0.56 µM in a β-arrestin recruitment assay using CHO cells expressing the human receptor).^1,2 It is selective for GPR18 over GPR55, as well as cannabinoid 1 (CB₁) and CB₂ receptors, at 10 µM but also binds to the adenosine A_2A receptor (K_i = 0.33 µM for the rat receptor).^1,3

WARNING This product is not for human or veterinary use.

1. Schoeder, C.T., Kaleta, M., Mahardhika, A.B., et al. Structure-activity relationships of imidazothiazinones and analogs as antagonists of the cannabinoid-activated orphan G protein-coupled receptor GPR18. Eur. J. Med. Chem. 155, 381-397 (2018).

2. Schoeder, C.T., Mahardhika, A.B., Drabczyńska, A., et al. Discovery of tricyclic xanthines as agonists of the cannabinoid-activated orphan G‑protein-coupled receptor GPR18. ACS Med. Chem. Lett. (2020).

3. Drabczyńska, A., Müller, C.E., Schiedel, A., et al. Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: Structure-activity relationships as adenosine A₁ and A_2A receptor ligands. Bioorg. Med. Chem. 15(22), 6956-6974 (2007).