Fig. 7: Proposed mechanisms of antagonist and agonist drugs.
From: Cryo-EM structures of ρ1 GABAA receptors with antagonist and agonist drugs
a Cartoons of ρ1 showing progressive ECD rotation between resting (green), partially-locked (purple) and activated (open or desensitized, blue) states. Loop C is highlighted, and GABA and ions are shown in circles (carbon, tan; amine, blue; carboxylate, red; chloride, green). b Cartoon zoom view of the orthosteric binding site. GABA is shown in circles as in (a). Green and blue lines depict lockdown of loop C. c Proposed dependence of orthosteric-site expansion/compaction on ligand identity, from antagonists to strong agonists.
