New Tricyclic γ-Aminobutyric Acid Analogue HSK16149: A Ca 2+ Channel α 2 -δ Ligand for Treating Neuropathic Pain

= 3.96 nM) and an AUC of 13,200 ng·h/mL which was obviously higher than the control drug pregabalin. HSK16149 also demonstrated superior antihypersensitivity or antiallodynic/hyperalgesic effects compared to the commonly used pregabalin as the control and has the potential to minimize CNS side effects with good tolerability. Based on its exceptional preclinical characteristics, HSK16149 was chosen for further development to provide a more effective and safer drug for patients enduring neuropathic pain.