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GABAa receptor-positive modulators are well-known to induce sedation, sleep, and general anesthesia. Conversely, GABAa receptor-negative allosteric modulators (GABAaRNAMs) can increase arousal and induce seizures. Motivated by their studies with patients with hypersomnia, and the discovery that two GABAaRNAMs can restore the Excitation/Inhibition balance in vitro and arousal in vivo, this research team chose to screen 11 compounds that have been reported to modulate arousal, to see if they shared a GABA-related mechanism. The computational modeling of modulator–receptor interactions predicted drug action at canonical binding sites and novel orphan sites on the receptor. The findings of the study suggest that multiple avenues of investigation are now open to investigate large and brain-penetrant molecules for the treatment of patients with diminished CNS E/I balance. Reference: Kaplan et al (2023) Commonly Used Therapeutics Associated with Changes in Arousal Inhibit GABAaR Activation. Biomolecules. 2023 Feb 15;13(2):365. doi: Guest: Professor Asher Brandt, Department of Chemistry, University of Saint Joseph Nanome is the ultimate interface for scientific discovery, starting with molecular data. Top R&D labs conduct cutting-edge research and make billion-dollar decisions in Nanome. But, Nanome isn’t just for experts, it’s also used by students and amateur scientists studying chemistry and biology. Anyone can build 3D molecules or simulate an entire protein made of hundreds of atoms, all in one collaborative environment. Transform the way you learn, design, and communicate molecular structures with Nanome. Available on the new Meta Quest Pro. Visit to download Nanome Get started today by downloading Nanome for free on: 1Oculus Rift/Rift S/Quest Link: SteamVR: Viveport App Lab: SideQuest: To learn more visit: or, follow us on: Twitter & Insta: @nanome_inc Be sure to also check out our blockchain platform, Matryx, which will serve as the backend IP tracking mechanism for Nanome. More info at
