380560-89-4
Chemical Structure
DQP-1105
- CAS No.: 380560-89-4
- Formula:C29H24BrN3O4
- Molecular Weight:558.42
IUPAC Name: 4-(5-(4-bromophenyl)-3-(6-methyl-2-oxo-4-phenyl-1,2-dihydroquinolin-3-yl)-4,5-dihydro-1H-pyrazol-1-yl)-4-oxobutanoic acid
InChIKey: MVYNQMRZRULRIE-UHFFFAOYSA-N
SMILES: O=C(CCC(N1N=C(CC1C2=CC=C(C=C2)Br)C3=C(C4=CC=CC=C4)C5=C(C=CC(C)=C5)NC3=O)=O)O
Biological Activity: DQP-1105 is a potent and selective NMDA receptor antagonist. DQP-1105 inhibits NMDA receptors containing GluN2C and GluN2D with IC50 values of 7.0 and 2.7 μM, respectively, and shows weaker inhibitory activity against receptors containing GluN2A or GluN2B. DQP-1105 exhibits higher affinity after the receptor binds glutamate, and inhibits high-frequency excitatory synaptic transmission by altering receptor gating kinetics or prolonging deactivation time. DQP-1105 can be used in research on epilepsy, depression, schizophrenia, and fragile X syndrome[1][2][3][4][5][6][7][8].
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DQP-1105 | 98.05% | DQP-1105 is a potent and selective NMDA receptor antagonist. DQP-1105 inhibits NMDA receptors containing GluN2C and GluN2D with IC50 values of 7.0 and 2.7 μM, respectively, and shows weaker inhibitory activity against receptors containing GluN2A or GluN2B. DQP-1105 exhibits higher affinity after the receptor binds glutamate, and inhibits high-frequency excitatory synaptic transmission by altering receptor gating kinetics or prolonging deactivation time. DQP-1105 can be used in research on epilepsy, depression, schizophrenia, and fragile X syndrome. | ||||||||||||||||||||
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References
- [1]. Brancaccio M, et al. Cell-autonomous clock of astrocytes drives circadian behavior in mammals. Science. 2019 Jan 11;363(6423):187-92.
- [2]. D'Erasmo MP, et al. Development of a Dihydroquinoline-Pyrazoline GluN2C/2D-Selective Negative Allosteric Modulator of the -Methyl-d-aspartate Receptor. ACS chemical neuroscience. 2023 Sep 06;14(17):3059-3076. [Content Brief]
- [3]. Brancaccio M, et al. Astrocytes Control Circadian Timekeeping in the Suprachiasmatic Nucleus via Glutamatergic Signaling. Neuron. 2017 Mar 22;93(6):1420-1435.e5.
- [4]. Gao R, et al. NMDAR (2C) deletion in astrocytes relieved LPS-induced neuroinflammation and depression. International Immunopharmacology. 2024 May 10;132:111964. [Content Brief]
- [5]. Zhou R, et al. Cerebellar GluN2C protects against sleep deprivation-induced cognitive impairment and motor incoordination. Sleep medicine. 2026 Jan;137:108648. [Content Brief]
- [6]. Shelkar GP, et al. Cocaine preference and neuroadaptations are maintained by astrocytic NMDA receptors in the nucleus accumbens. Science Advances. 2022 Jul 22;8(29):eabo6574.
- [7]. Gawande DY, et al. GluN2D Subunit in Parvalbumin Interneurons Regulates Prefrontal Cortex Feedforward Inhibitory Circuit and Molecular Networks Relevant to Schizophrenia. Biological psychiatry. 2023 Aug 15;94(4):297-309.
- [8]. Shedd A, et al. A cell type-specific switch in GluN2D NMDA receptors drives cortical circuit hyperexcitability and sensory-driven cortical synchronization deficits in a Fragile X Syndrome model. Biological psychiatry. 2026 Sep 21.