Adaptaquin

Adaptaquin is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2; IC₅₀ = 2 micromolar).¹ It stabilizes HIF-1α protein and induces expression of the HIF-1-regulated genes EPO and VEGF in SH-SY5Y human neuroblastoma cells. Adaptaquin protects against cell death induced by glutathione depletion in rat primary cortical neurons (IC₅₀ = 0.25 μM) and reduces glutamate-induced cell death in HT-22 cells.^1,2 In vivo, adaptaquin (30 mg/kg) increases pellet retrieval in the single-pellet reaching task in a rat autologous striatal blood infusion model of intracerebral hemmorhage and normalizes preference for ipsilateral turns in a mouse model of striatal hemorrhage.³

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1. Smirnova, N.A., Rakhman, I., Moroz, N., et al. Utilization of an in vivo reporter for high throughput identification of branched small molecule regulators of hypoxic adaptation. Chem. Biol. 17(4), 380-391 (2010).

2. Neitemeier, S., Dolga, A.M., Honrath, B., et al. Inhibition of HIF-prolyl-4-hydroxylases prevents mitochondrial impairment and cell death in a model of neuronal oxytosis. Cell Death Dis. 7, e2214 (2016).

3. Karuppagounder, S.S., Alim, I., Khim, S.J., et al. Therapeutic targeting of oxygen-sensing prolyl hydroxylases abrogates ATF4-dependent neuronal death and improves outcomes after brain hemorrhage in several rodent models. Sci. Transl. Med. 8(328), (2016).