Fig. 1: Quinazolinones act as positive allosteric modulators through binding to TMD sites in the α1β2γ2 GABAA receptor. | Nature Communications

Fig. 1: Quinazolinones act as positive allosteric modulators through binding to TMD sites in the α1β2γ2 GABAA receptor.

From: Structural insights into GABAA receptor potentiation by Quaalude

Fig. 1: Quinazolinones act as positive allosteric modulators through binding to TMD sites in the α1β2γ2 GABAA receptor.

a Exemplary whole-cell patch-clamp electrophysiology trace showing the PAM and agonist activities displayed by methaqualone (MQ) and PPTQ on the EM receptor at their respective EC50 concentrations; n = 6 recordings from independent cells; GABA EC10 = 4 µM. b and c EM density map showing two methaqualone binding sites per receptor. b Side view of the receptor. c Cross section through the transmembrane domain and ligand chemical structure. d and e Same as b and c for PPTQ.

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