2-PMPA 是一种有效的(IC50 ~ 1 nM)选择性谷氨酸羧肽酶 II(GCPII)抑制剂,也称为 N-乙酰基-L-天冬氨酰-L-谷氨酸肽酶 I(NAALADase I)、NAAG 肽酶或前列腺素-特异性膜抗原(PSMA)。2-PMPA 具有神经保护活性。2-PMPA 在多发性硬化症的 EAE 模型中已被证明可预防和治疗认知障碍,并防止梭曼诱导的神经病理学。 2-PMPA 是谷氨酸羧肽酶 II(GCPII)的有效选择性抑制剂。 2-(膦酰基甲基)戊二酸(2-PMPA)阻断由低单位剂量的可卡因维持的静脉内可卡因自我给药。此外,它还抑制可卡因诱导的寻求毒品行为的恢复。2-PMPA 可降低麻醉小鼠脑内血氧水平依赖(BOLD)信号。2-PMPA is a potent and selective inhibitor of Glutamate carboxypeptidase II (GCPII).
2-(phosphonomethyl)pentanedioic acid (2-PMPA) blocks intravenous cocaine self-administration maintained by low unit doses of cocaine. In addition, it also inhibits cocaine-induced reinstatement of drug-seeking behavior. 2-PMPA reduces blood oxygen-level dependent (BOLD) signals in brain of anesthetized mice.
2-PMPA is a potent (IC50 ~ 1 nM) and selective inhibitor of Glutamate carboxypeptidase II (GCPII), also known as N-acetyl-L-aspartyl-L-glutamate peptidase I (NAALADase I), NAAG peptidase, or prostate-specific membrane antigen (PSMA). 2-PMPA has neuroprotective activity activity. 2-PMPA has been shown to prevent and treat cognitive impairment in the EAE model of multiple sclerosis and to protect against soman-induced neuropathology.