The present invention relates to the field of pharmaceutical chemistry. In particular, the present invention relates to a γ-aminobutyric acid type-B receptor (Gamma Aminobutyric Acid B Receptor, referred to as a GABABR or GABAB receptor for short) ligand molecule and a medicinal use thereof, wherein the ligand molecule has the structure of formula I. The ligand molecule which the present invention relates to is a GABAB receptor negative allosteric modulator, can non-competitively inhibit GABAB receptor agonist-induced activation of the receptor, and can be used to prepare drugs for the treatment of GABAB receptor hyperexcitability-related diseases, wherein the diseases comprise epilepsy, anxiety, depression or low cognitive ability caused by nerve damage, and so on.
GABAB RECEPTOR NEGATIVE ALLOSTERIC MODULATOR AND MEDICAL USE THEREOF