Use of a GABAA receptor allosteric enhancer in medicine

#This application is a National Stage of International Application No. PCT/CN2019/095395, filed Jul. 10, 2019, which claims priority to Chinese Patent Application No. 201811011320.1, filed Aug. 31, 2018, both of which are hereby incorporated by reference in their entireties.

#This disclosure relates to the field of medicine, specifically, to the use of a GABAA receptor allosteric enhancer in medicine.

#Epilepsy is a chronic condition in which sudden abnormal discharge of neurons in the brain causes transient brain dysfunction. Seizures are clinical phenomena caused by brain neuron abnormality and excessive hyper-synchronized discharge. Due to the increasing prevalence of epilepsy patients in China and abroad, epilepsy is a growing health concern in the society. Statistics show that epilepsy sufferers account for about 0.5% to 1% of the world's population. Despite of ongoing and in-depth studies of epilepsy, little is known about the pathogenesis of epilepsy, while the drugs currently used only partially relieve the condition of patients with epilepsy and are only 60 to 70 percent effective in patients with developing major episodes.

#FIG. 1 is a diagram of the changes in Compound 1 and dipropofol concentrations in brain tissues at different points in time after administration in rats.

#FIG. 2 provides the number of spontaneous seizure episodes in the KA-induced chronic epilepsy model in Experimental Example 1.

#FIG. 3 is the neuronal cell survival rate of the KA-induced chronic epilepsy model in Experimental Example 1.

#The technical solutions of the present disclosure will be described in details below in conjunction with the accompanying drawings and examples and are encompassed by, but not limiting the protection scope of this disclosure.

#(1) In a 25 mL round bottom flask, o-isopropyl phenol (1.0 g, 7.3 mmol) and allyl bromide (14.6 mmol) were consecutively added and dissolved with dichloromethane;

#(2) In another 50 mL flask, benzyl tributyl ammonium bromide (0.26 g, 0.73 mmol) was added and dissolved with a 1M NaOH solution;