D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 inhibits the glutamate binding site of NMDA receptors[1][2].
D-AP5 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Mouse cerebral artery endothelial cells
10 µM
10 minutes
D-AP5 significantly prevented the NMDA-induced increase in NMDAR sparklets, indicating that D-AP5 inhibits Ca2+ signaling by blocking the glutamate binding site of NMDAR.
J Cereb Blood Flow Metab. 2022 Jan;42(1):145-161.
Cortical wedges
3.7 ± 0.32 µM (IC50)
15-20 minutes
D-AP5 exhibited a selective reduction of NMDA-induced depolarization in cortical wedges with little or no effect on responses to quisqualate or kainate.
Br J Pharmacol. 1988 Nov;95(3):957-65.
Mouse motor cortex slices
100 µM
25 minutes
D-AP5 facilitated uniform DCS-LTD across the cortical thickness, abolishing DCS-LTP in deep layers
Ann Neurol. 2020 Sep;88(3):489-502.
D-AP5 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
Cecal ligation puncture (CLP)-induced sepsis model
Bilateral injection
1 μg/μl
Single injection, lasting 30 minutes
D-AP5 significantly prevented CNO-induced memory consolidation and improved cognitive dysfunction in septic mice.
CNS Neurosci Ther. 2023 Jan;29(1):390-401
Mice
C57bl6/J mice
In vitro perfusion
10 mmol/L
Single administration, lasting 10 minutes
D-AP5 significantly blunted NMDA-induced dilation of PComA and parenchymal arterioles, indicating that D-AP5 attenuates vasodilation by inhibiting NMDAR in endothelial cells.
J Cereb Blood Flow Metab. 2022 Jan;42(1):145-161.
Mice
Mouse kainic acid seizure model
Intraperitoneal injection
300μM
Single dose, 60 minutes duration
D-AP5 abolished DCS-LTP in deep layers, enhancing the uniformity of DCS-LTD
Ann Neurol. 2020 Sep;88(3):489-502.
Rats
Spinal and brainstem neurones
Intravenous injection
50-100 mg/kg
Single injection, effects lasted more than 6 hours
D-AP5, administered intravenously, selectively reduced NMDA-induced excitation in rat spinal and brainstem neurones, with effects lasting more than 6 hours.
Br J Pharmacol. 1988 Nov;95(3):957-65.
D-AP5 动物研究
Animal study
D-AP5, an antagonist of NMDA receptors, has been observed to disrupt spatial learning and long-term potentiation (LTP) in a dose-dependent manner when administered chronically via intraventricular infusion. Notably, intracerebral D-AP5 does not cause sensorimotor disturbances when it prevents spatial learning[2]. Furthermore, D-AP5 treatment leads to a gradual decrease in swimming speed across trials. It also induces sensorimotor disruptions in spatial tasks, which worsen as the learning impairment progresses. In delayed matching-to-place water maze tests, rats receiving D-AP5 exhibit a delay-related decline in spatial memory[3].
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