2055045-42-4
Chemical Structure
JWX-A0108
- CAS No.: 2055045-42-4
- Formula:C19H14ClFN4OS
- Molecular Weight:400.86
InChIKey: HLGMORDKLMTTGN-UHFFFAOYSA-N
SMILES: O=C1C2=C(N=CN1C3=C(C)C=CC=C3Cl)N=C(NC4=CC=C(C)C(F)=C4)S2
Biological Activity: JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC50 of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease[1][2][3].
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JWX-A0108 | JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC50 of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease. | |||||||||||||||||||||
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- [1]. Sun LL, et al. Pharmacological characterization of JWX-A0108 as a novel type I positive allosteric modulator of α7 nAChR that can reverse acoustic gating deficits in a mouse prepulse inhibition model. Acta Pharmacol Sin. 2019;40(6):737-745. [Content Brief]
- [2]. Li H, et al. JWX-A0108, a positive allosteric modulator of α7 nAChR, attenuates cognitive deficits in APP/PS1 mice by suppressing NF-κB-mediated inflammation. Int Immunopharmacol. 2021;96:107726. [Content Brief]
- [3]. Sun L, et al. Pharmacological Properties and Evaluations of a Novel Positive Allosteric Modulator of α7 nAChR for Attenuation of Schizophrenia-Like Behavior in Mice. Published in: Volume 114, Issue 3, Supplement 1, page 297A, February 2, 2018.
Keywords
