Approaches to anxioselective GABAa receptor modulators

Two approaches have been taken in the pursuit of improved anxiolytic compounds acting via the BZ receptor. Compounds with partial efficacy as positive allosteric modulators could elicit anxiolytic effects with a reduced propensity for sedation and amnesia. This approach assumes that only a limited degree of GABAA receptor potentiation is required to produce anxiolysis, whereas a greater potentiation is necessary to produce side effects. The second approach is focused on developing a positive allosteric modulator selective for a2- (and/or a3-) subunit-containing GABAA receptors that would be anxiolytic lacking the sedative, amnestic, and tolerance properties of classical BZ ligands. These two approaches are not mutually exclusive and a compound with combined subtype selectivity and partial efficacy may be a superior anxiolytic. The challenge of finding such compounds has been such that no anxioselective BZs have advanced to the market.82,102,111

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