Ogerin

Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC₅₀=6.83) with a moderate antagonistic effect on A_2A (K_i=220 nM). Ogerin inhibits the fear conditioning reflex in mice and also inhibits TGF-β-induced myofibroblast differentiation of fibroblasts from multiple organ systems. Ogerin can be used in the studies of fibrotic diseases and neurological disorders^[1][2]. IC50 & Target:pEC50: 6.83 (GPR68)^[1]
Ki: 220 nM (A_2A receptoor), 736 nM (5-HT_2B receptor)^[1] In Vitro:Ogerin (50-150 μM; 72 h) inhibits and partially reverses TGF-β induced pro-fibrotic fibroblast phenotypes in PHLFs^[1].
Ogerin (50-150 μM; 48 h) inhibits basal and TGF-β induced collagen production at the transcriptional level in PHLFs^[1].
Ogerin (50, 100 μM; 72 h) shows anti-proliferative effect on TGF-β stimulated PHLFs^[1].
Ogerin (150 μM; 40 min) activates Gα_s signaling in PHLFs^[1].
Ogerin (50 μM; 10 min) activates the PKA and MAP kinase pathways in HEK293 cells (stably expressing HA-GPR68)^[2]. In Vivo:Ogerin (10 mg/kg; single) shows effects that supports a role for GPR68 in hippocampal-associated memory^[2].