Ifenprodil (+)-tartrate salt (hemitartrate salt)

Ifenprodil tartrate, Ifenprodil hemitartrate
An Antagonist of NMDA Receptors
    Cat #: I-105
    Alternative Name Ifenprodil tartrate, Ifenprodil hemitartrate
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 801
    Purity: >98%
    Form Lyophilized powder.
    Effective concentration 0.1-100 µM.
    Structure
    • Ifenprodil (+)-tartrate salt (hemitartrate salt)
    Chemical name 4-[2-(4-benzylpiperidin-1-yl)-1-hydroxypropyl]phenol;2,3-dihydroxybutanedioic acid OR α-(4-Hydroxyphenyl)-β-methyl-4-benzyl-1-piperidineethanol (+)-tartrate salt.
    Molecular formula C46H60N2O10.
    CAS No.: 23210-58-4.
    PubChem CID 11957579
    Activity Ifenprodil inhibits NMDA receptors with the following IC50s: 0.15 μM (NR2B), 39 μM (NR2A), 29 μM (NR2C)1.
    References-Activity
    1. Traynelis, S.F. et al. (2010) Pharmacol. Rev. 62, 405.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Up to 10 mM in water or ethanol. Centrifuge all product preparations before use (5,000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Ifenprodil (+)-tartrate salt (hemitartrate salt)
      Alomone Labs Ifenprodil (+)-tartrate salt (hemitartrate salt) inhibits NMDA (NR1+NR2A) channels expressed in Xenopus oocytes. 
      A. Time course of NMDA currents elicited with 100 µM glutamate and 100 µM Glycine, every 50s, while membrane potential was held at -80 mV. 100 µM Ifenprodil (+)-tartrate salt (hemitartrate salt) (#I-105), applied for 3 min, as indicated, reversibly inhibited current amplitude. B. superimposed current traces taken from the experiment described in A.
    References - Scientific background
    1. Han, X. et al. (2008) J. Neurochem. 107, 1566.
    2. Traynelis, S.F. et al. (2010) Pharmacol. Rev. 62, 405.
    3. Kew, J,N. et al. (1996) J. Physiol. 497, 761.
    4. Mony, L. et al. (2009) Br. J. Pharmacol. 157, 1301.
    Scientific background

    Ifenprodil is an atypical, selective, noncompetitive, voltage-independent partial antagonist of N-methyl-D-aspartate (NMDA) receptors. Its maximal inhibition is approximately at 90%. Ifenprodil inhibits GluN2B-containing receptors with high affinity and is more potent for GluN1/GluN2B receptors. Ifenprodil action is pH-dependent and may cause an increase in tonic proton inhibition. There is evidence that ifenprodil binds outside the ion channel pore to the large interlobe cleft of the NR2B N-terminal domain and acts at a discrete sites with an allosteric interaction. Mutations at distinct residues in the R domain of NR1 and NR2B greatly influence ifenprodil inhibition, thus it seems that this region may form part of the ifenprodil binding site1-3. IC50 values of ifenprodil are 0.15 μM for NR2B subunit, 39 μM for NR2A, 29 μM for NR2C and 76 μM for NR2D2.

    NMDA receptors are gated ion channels by glutamate and are involved in numerous physiological and pathological processes including synaptic plasticity, chronic pain and psychosis4.

    Ifenprodil has neuroprotective abilities in in vivo models of cerebral ischemia and has the ability to protect cultured neurons from NMDA mediated toxicity without many of the side effects caused by NMDA antagonist3.

    Ifenprodil was proven to be a useful pharmacological tool to study the structure and function of NMDA receptors. Ifenprodil rise pharmaceutical interest because of its therapeutic potential for neurological and psychiatric disorders such as treating pain4.

    Target NMDA receptors
    Last update: 24/01/2020

    Ifenprodil (+)-tartrate salt (hemitartrate salt) (#I-105) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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