New High-Resolution Structures with Salipro® to Enable Safer Sedatives Development

In a recent study published in Nature Communications by Ryan Hibbs and his team, Salipro® enabled high-resolution cryoEM structures of the GABAA receptor with the sedatives Methaqualone and its derivative, PPTQ, revealing the GABAA receptor binding sites for quinazoline family drugs.

Methaqualone, known as Quaalude, was used clinically as a sedative-hypnotic. However, its high abuse potential led to the prohibition of its medical use, leaving its pharmacology understudied.

Together with Salipro®, these new findings provide never-before-seen 3D insights into how these drugs interact with the receptor and pave the way for the design of a new generation of quinazoline analogs with limited abuse potential. 

Find more information about the study:  
W. Chojnacka, et al., Structural insights into GABAA receptor potentiation by Quaalude. Nat. Commun. 15, 5244 (2024).