Cipepofol

Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABA_A receptor. Cipepofol can cause the central nerve inhibition and promote sleep based on the structural modification of Propofol (HY-B0649). Cipepofol can activate the sirtuin1 (Sirt1)/Nrf2 pathway. Cipepofol protects the heart against Isoproterenol (ISO; HY-B0468)-induced myocardial infarction by reducing cardiac oxidative stress, inflammatory response and cardiomyocyte apoptosis^[1][2]. In Vitro:Cipepofol (Ciprofol) can trigger chloride influx by competitive binding to butylbicyclophosphorothionate and t-butylbicycloorthobenzoate targets in the chloride channels of GABAA receptors. The influx of chloride can cause hyperpolarization of nerve cell membranes by increasing the intracellular chloride concentration and further activating GABAergic neurons to achieve central nerve inhibition^[1].
Cipepofol (5 μM before ISO insult for 6 h) blunts the contents of CK-MB, LDH and cTnT were increased in ISO-treated H9c2 cells. Cipepofol attenuates ISO-induced cardiomyocyte apoptosis in vitro^[2].
In Vivo:Cipepofol (Ciprofol; 100 μL; implanted into the abdomen of mice 1 h before ISO) suppresses ISO-induced myocardial damage, cardiac dysfunction, and inflammation and cardiomyocyte apoptosis^[2].