2-PMPA

2-PMPA (2-(Phosphonomethyl)pentanedioic acid) is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC₅₀ of 0.0003 μM. 2-PMPA shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA is applicable to the research of neurological diseases^[1][2]. In Vitro:2-PMPA remains stable in rat plasma when stored at room temperature for 4 h, subjected to 3 freeze-thaw cycles, stored at -80°C for 28 days, and placed in a 10°C autosampler for 18 h^[2]. In Vivo:2-PMPA (167-250 mg/kg; intraperitoneal injection; single dose) induces a dose-dependent biphasic BOLD signal response in the gray matter of anesthetized mice, with a sustained signal decrease of 2.15-4.64% at 250 mg/kg and a transient signal decrease of 1% at 167 mg/kg^[1].
2-PMPA (80 mg/kg; i.p.; single dose) exerts no significant effects on motor coordination or cognitive ability in Swiss-Webster mice within 24 hours^[1].
2-PMPA (100 mg/kg; intraperitoneal injection; single dose) is rapidly absorbed in male Wistar rats, with low brain penetration (a brain/plasma AUC_0-t ratio of 0.018), while it shows higher penetration in peripheral nerve tissues^[2].