GABAA receptor modulator-9 is a positive allosteric modulator of the GABAA receptor, specifically targeting the alpha1beta2gamma2 subtype and capable of crossing the blood-brain barrier. It exhibits excellent activity at alpha1beta2gamma2 (EC50: 0.9 µM in oocytes and 0.2 µM in CHO cells) and also shows activity at alpha1beta2, alpha3beta2gamma2, and alpha1beta3gamma2 (with EC50 values of 1.3, 3.4, and 1.1 µM, respectively). GABAA receptor modulator-9 significantly inhibits seizure progression and reduces mortality in mice. It is applicable in studies of status epilepticus (SE).
Target-Kategorie:
GABA Receptor
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