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A positive allosteric modulator of α2- and α3 subunit-containing GABAA receptors
AZD 7325 is a positive allosteric modulator of α2- and α3 subunit-containing GABAA receptors and a neutral antagonist for α1 subunit-containing GABAA receptors.1 It binds to GABAA receptors in membranes from Sf9 cells expressing α2β3γ2 subunit-containing receptors (Ki = 0.309 nM). AZD 7325 (1 mg/kg) increases marble-burying behavior, indicating anxiety-like activity, and decreases audiogenic seizure severity in the Fmr1-/- mouse model of fragile X syndrome.2
1.Alhambra, C., Becker, C., Blake, T.A., et al.Development and SAR of functionally selective allosteric modulators of GABAA receptorsBioorg. Med. Chem.19(9)2927-2938(2011) 2.Schaefer, T.L., Ashworth, A.A., Tiwari, D., et al.GABAA alpha 2,3 modulation improves select phenotypes in a mouse model of fragile X syndromeFront. Psychiatry12678090(2021)
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