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In vitro: 2-PMPA (PMPA tetrasodium salt) is a potent and selective inhibitor of GCPII, an enzyme which catabolizes the abundant neuropeptide N-acetyl-aspartyl-glutamate (NAAG) to N-acetylaspartate (NAA) and glutamate. 2-PMPA demonstrates robust efficacy in numerous animal models of neurological disease. 2-PMPA is a highly polar compound with multiple negative charges causing significant challenges for analysis in biological matrices.
In vivo: Intraperitoneal administration of 100 mg/kg 2-PMPA results in maximum concentration in plasma of 275 μg/mL at 0.25 h. The half-life, area under the curve, apparent clearance, and volume of distribution are 0.64 h, 210 μg×h/mL, 7.93 mL/min/kg, and 0.44 L/kg, respectively. 2-PMPA at 250 mg/kg, in an anesthetized mouse, after an initial rise, produces a rapid decline and a striking attenuation in BOLD signals in gray matter. The signature of 2-PMPA on brain T2* signals in gray matter at both 167 and 250 mg/kg includes a significant initial rise lasting several minutes.
CAS#: 173039-10-6(free base)
Front Cell Dev Biol. 2021 Mar 4;9:598377.
Prostate-Specific Membrane Antigen (PSMA) Promotes Angiogenesis of Glioblastoma Through Interacting With ITGB4 and Regulating NF-κB Signaling Pathway
2-PMPA tetrasodium purchased from AbMole
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Source | Front Cell Dev Biol (2021 Mar). Figure 3. 2-PMPA (Abmole Bioscience, USA) |
| Method | Cell Culture | |
| Cell Lines | HUVECs, U87 and U251 cell lines | |
| Concentrations | 100 µM | |
| Incubation Time | 24 h | |
| Results | Meanwhile, the treatment of PSMA inhibitor 2-PMPA could effectively eliminate PSMA expression in all groups |
| Cell Experiment | |
|---|---|
| Cell lines | Neuronal cultures |
| Preparation method | 2-PMPA is selected to explore the protective effect on ketamine-induced neurotoxicity in these two different cell cultures. Cells are exposed to 2-PMPA (20, 50, 100 μM) half an hour before 10 μM ketamine treatment in neuronal cultures and 2 mM ketamine treatment in neuron–glia mixed cultures for 24 h. Different doses of ketamine chosen in neuronal cultures and neuron–glia mixed cultures are based on the results of cell viability tests. |
| Concentrations | 20, 50, 100 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Male Wistar rats |
| Formulation | 50 mM HEPES buffered saline |
| Dosages | 80 mg/kg |
| Administration | i.p. |
| Molecular Weight | 314.05 |
| Formula | C6H7Na4O7P |
| CAS Number | 373645-42-2 |
| Solubility (25°C) | Water ≥ 10 mg/mL |
| Storage | 4°C, dry, sealed |
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