3103822-75-6
Chemical Structure
GABAA receptor modulator-14
- CAS No.: 3103822-75-6
- Formula:C22H13F2N5O2S
- Molecular Weight:449.43
InChIKey: QONNFFKOVHWKFU-UHFFFAOYSA-N
SMILES: O=C1C2=C(N=C(N1C3=CC(F)=CC(F)=C3)C4=CC=CC=C4)N=C(C5=CN=C(N=C5)OC)S2
Biological Activity: GABAA receptor modulator-14 is an orally active, blood-brain barrier permeable selective positive allosteric modulator (PAM) of extrasynaptic δ-containing GABAA receptors (α4β3δ subtype) with an EC50 of 0.8 μM. GABAA receptor modulator-14 selectively enhances tonic neuronal inhibition by potentiating GABA-evoked currents mediated by extrasynaptic δ-GABAARs, produces rapid sustained antidepressant effects, elevates slow-wave NREM sleep and shows no addiction liability in mice. GABAA receptor modulator-14 can be applied to major depressive disorder (MDD) and comorbid insomnia research[1].
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GABAA receptor modulator-14 | GABAA receptor modulator-14 is an orally active, blood-brain barrier permeable selective positive allosteric modulator (PAM) of extrasynaptic δ-containing GABAA receptors (α4β3δ subtype) with an EC50 of 0.8 μM. GABAA receptor modulator-14 selectively enhances tonic neuronal inhibition by potentiating GABA-evoked currents mediated by extrasynaptic δ-GABAARs, produces rapid sustained antidepressant effects, elevates slow-wave NREM sleep and shows no addiction liability in mice. GABAA receptor modulator-14 can be applied to major depressive disorder (MDD) and comorbid insomnia research. | |||||||||||||||||||||
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