中文名 | 2-PMPA |
英文名 | 2-(Phosphonomethyl)pentanedioic acid |
别名 | 化合物2-PMPA 2-PMPA游离态 2-(膦酰基甲基)戊二酸 NAALADASEINHIBITOR(易潮) |
英文别名 | 2-PMPA CS-2454 NAALADASEINHIBITOR PMPA(NAALADaseinhibitor) 2-PMPA(NAALADaseinhibitor) 2-(Phosphonomethyl)pentanedioic acid 2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID Pentanedioic acid, 2-(phosphonomethyl)- 2-(Phosphonomethyl)pentane-1,5-dioicacid 2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID (PMPA) |
CAS | 173039-10-6 |
化学式 | C6H11O7P |
分子量 | 226.12 |
密度 | 1.658±0.06 g/cm3(Predicted) |
沸点 | 538.8±60.0 °C(Predicted) |
酸度系数 | 2.06±0.10(Predicted) |
存储条件 | room temp |
外观 | 粉末 |
颜色 | white to beige |
体外研究 | 2-PMPA 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. 2-PMPA reduces ketamine-induced decrease of cell viability and increase of LDH levels in the mixed cultures but not in the neuronal cultures. |
体内研究 | 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 T 2 * signals in gray matter at both 167 and 250 mg/kg includes a significant initial rise lasting several minutes. 2-PMPA has neuroprotective activity in an animal model of stroke and anti-allodynic activity in CCI model. Administration of 2-PMPA (50mg/kg) produces a mean peak concentration of 2-PMPA of 29.66±8.1 μM. This concentration is about 100,000 fold more than is needed for inhibition of NAAG peptidase, and indicates very good penetration to the brain. Administration of 50 mg/kg 2-PMPA (i.p.) produces a continuously increasing extracellular NAAG concentration, which startes directly after application. |
RTECS | SA0454800 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.422 ml | 22.112 ml | 44.224 ml |
5 mM | 0.884 ml | 4.422 ml | 8.845 ml |
10 mM | 0.442 ml | 2.211 ml | 4.422 ml |
5 mM | 0.088 ml | 0.442 ml | 0.884 ml |
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