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PMPA (NAALADase inhibitor)

Catalog No.
A4414
Glutamate carboxypeptidase 2 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$95.00
Ship with 10-15 days
10mg
$158.00
Ship with 10-15 days
25mg
$315.00
Ship with 10-15 days
50mg
$459.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

PMPA is a selective inhibitor of NAALADase with Ki value of 275 pM [1].
NAALADase also known as GCPII is a zinc metalloenzyme that resides in membranes and involves in the catalyzing process of neuropeptide NAAG to NAA and glutamate. It has been shown that NAALADase has the highest expression in nervous/ prostatic tissues and cancers and NAALADase inhibition produces a variety of effects on providing neuroprotection, detection, imaging and treatment of prostate cancer [2] [3].
PMPA is a potent NAALADase inhibitor and has a more activity than reported NAALADase inhibitor ZJ43. In male C57/Bl mice model, high doses of PMPA inhibited the morphine tolerance development (resembling the effect of 7.5 mg/kg of the NMDA receptor antagonist, memantine) while had no effect on severity of withdrawal; 100 mg/kg PMPA also significantly potentiated morphine withdrawal, but inhibited both acquisition and expression of morphine-induced conditioned place preference which suggested NAALADase involves in phenomena related to opioid addiction [4]. PMPA treatment increased the mice latency to enter the dark box during the training day and at the dose of 150 mg/kg PMPA treatment impaired spontaneous alternation and reduced locomotion in Y-maze task which demonstrated that PMPA affected mice learning and memory tasks through NAALADase inhibition [5].
References:
[1].    Tiffany, C.W., et al., Binding of the glutamate carboxypeptidase II (NAALADase) inhibitor 2-PMPA to rat brain membranes. Eur J Pharmacol, 2001. 427(2): p. 91-6.
[2].    Barinka, C., et al., Glutamate carboxypeptidase II in diagnosis and treatment of neurologic disorders and prostate cancer. Curr Med Chem, 2012. 19(6): p. 856-70.
[3].    Slusher, B.S., et al., Selective inhibition of NAALADase, which converts NAAG to glutamate, reduces ischemic brain injury. Nat Med, 1999. 5(12): p. 1396-402.
[4].    Popik, P., et al., Morphine tolerance and reward but not expression of morphine dependence are inhibited by the selective glutamate carboxypeptidase II (GCP II, NAALADase) inhibitor, 2-PMPA. Neuropsychopharmacology, 2003. 28(3): p. 457-67.
[5].    Lukawski, K., R.M. Kaminski, and S.J. Czuczwar, Effects of selective inhibition of N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) on mice in learning and memory tasks. Eur J Pharmacol, 2008. 579(1-3): p. 202-7.

Chemical Properties

Physical AppearanceWhite solid
StorageDesiccate at RT
M.Wt226.12
Cas No.173039-10-6
FormulaC6H11O7P
SolubilitySoluble to 100 mM in sterile water
Chemical Name2-(phosphonomethyl)pentanedioic acid
SDFDownload SDF
Canonical SMILESC(CC(=O)O)C(CP(=O)(O)O)C(=O)O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

PMPA (NAALADase inhibitor)