Norgestrel

Norgestrel is a synthetic analog of progesterone, a compound commonly found in oral contraceptive pill, and a powerful neuroprotective antioxidant, preventing light-induced ROS in photoreceptor cells, and cell death^[1][2]. Norgestrel is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. In Vitro: Norgestrel (20 μM; 24 hours; 661W cells) treatment significantly increases cellular viability after serum deprivation and so it is demonstrated that Norgestrel is neuroprotective to stressed 661W cells^[1].
Norgestrel (20 μM; 24 hours; 661W cells) treatment decreases apoptotic induced cleavage of PARP and caspase-3^[1].
Norgestrel (20 μM; 6 hours; 661W cells) treatment bFGF is results in a significant upregulation of bFGF mRNA in photoreceptor cells^[1]. In Vivo: Norgestrel (100 mg/kg; intraperitoneal injection; for 6, 24 or 48 hours; Balb/c mice) treatment can prevent light-induced ROS in photoreceptor cells, and subsequent cell death. Norgestrel acts via post-translational modulation of the major antioxidant transcription factor Nrf2; bringing about its phosphorylation, subsequent nuclear translocation, and increases levels of its effector protein superoxide dismutase 2 (SOD₂)^[2].