Cipepofol, a Sedative-Hypnotic Agent, is a GABA Receptor Potentiator

GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA). There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). As we all know, Bicuculline and Picrotoxin block the rapid response of neurons to GABA due to direct activation of anion channels. Propofol depresses heart rate and blood pressure through GABAA receptor–mediated effects on autonomic control in the brainstem. Propofol is one of the most widely used intravenous anesthetics in clinical practice. However, Propofol also has obvious disadvantages, including injection pain, decreased diastolic blood pressure and mean arterial blood pressure, and respiratory depression.

Cipepofol (also known as HSK3486), a sedative-hypnotic agent, is a short-acting gamma-aminobutyric acid (GABA) receptor potentiator. In addition, Cipepofol is a compound for the intravenous induction and maintenance of anesthesia. Recent research found that, Cipepofol rapidly induced sedation and anesthesia, with a smooth and rapid recovery. More importantly, Cipepofol can obviously improve the side effects (e.g., injection pain, respiratory depression, and decrease in blood pressure). Moreover, Cipepofol shows favourable pharmacokinetic characteristics, pharmacodynamic responses and safety at the study dose. After initial evaluations of absorption, distribution, metabolism, and excretion (ADME) processes, the Cmax, Tmax, T1/2, and mean residence time (MRT) are similar between Cipepofol and Propofol.

To sum up, Cipepofol, a sedative-hypnotic agent, is a short-acting gamma-aminobutyric acid (GABA) receptor potentiator similar to Propofol.


[1] Xiaojiao Li, et al. Front Pharmacol. 2021 Aug 27;12:735700.