PhTx-74

Philanthotoxin-7,4
Selective Antagonist of Various AMPA Receptors
    Cat #: P-120
    Alternative Name Philanthotoxin-7,4
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 507.54
    Purity: >99% (HPLC)
    Effective concentration 0.1-100 μM.
    Structure
    • PhTx-74
    Chemical name (S)-N-[7-[(4-Aminobutyl)amino]heptyl]-4-hydroxy-α-[(1-oxobutyl)amino]benzenepropanamide dihydrochloride.
    Molecular formula C24H44Cl2N4O3.
    CAS No.: 401601-12-5, 1227301-51-0.
    Activity PhTx-74 (Philanthotoxin-7,4) is a synthetic polyamine analogue of the naturally occurring wasp venom toxin philanthotoxin-4,3,3. It is a potent and selective antagonist of certain isoforms of the AMPA type of ionotropic glutamate receptors1. PhTx-74 inhibited GluR1 and GluR3 homomers as well as GluR1/GluR2 where 100 μM inhibited nearly 100% of the glutamate evoked currents. However, up to 500 μM had no or little effect on GluR2 or GluR2/GluR3 channels1-2.
    References-Activity
    1. Kromann, H. et al. (2002) J. Med. Chem. 45, 5745.
    2. Nilsen, A. and England, P.M. (2007) J. Am. Chem. Soc. 129, 4902.
    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 Water. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or six months at -20°C.
    Our bioassay
    • PhTx-74
      Alomone Labs PhTx-74 inhibits AMPA Receptor 1 (GluR1) expressed in Xenopus oocytes.
      Currents were recorded following stimulation with 10 µM glutamate (bar on top) at -100 mV holding potential. Reversible inhibitory effects of 0.1 to 10 µM of PhTx-74 (#P-120) are demonstrated, as indicated by the bars at the bottom.
    References - Scientific background
    1. Kromann, H. et al. (2002) J. Med. Chem. 45, 5745.
    2. Nilsen, A. and England, P.M. (2007) J. Am. Chem. Soc. 129, 4902.
    3. Lante, F. et al. (2011) J. Neurosci. 31, 3953.
    4. Argilli, E. et al.  (2008) J. Neurosci. 28, 9092.
    5. Jackson, A.C. et al.  (2011) J. Neurosci. 31, 7511.
    Scientific background

    PhTx-74 (Philanthotoxin-7,4) is a synthetic polyamine analogue of the naturally occurring wasp venom toxin philanthotoxin-4,3,3. It is a potent and selective antagonist of certain isoforms of the AMPA type of ionotropic glutamate receptors1.

    PhTx-74 inhibited GluR1 and GluR3 homomers as well as GluR1/GluR2 where 100 µM inhibited nearly 100% of the glutamate evoked currents. However, up to 500 µM had no or little effect on GluR2 or GluR2/GluR3 channels1-2.

    PhTx-74 (5 µM) was used as a tool to demonstrate circadian changes in AMPAR subtypes functionally expressed in somatosensory cortex slices and the removal of some AMPAR during sleep.

    Indeed, EPSPs were significantly depressed by PhTx-74 only after dark episodes3. As a measure for changes in AMPAR subunit composition after cocaine administration, PhTx-74 was used in synaptic transmission evaluation. AMPAR EPSCs from neurons treated earlier with cocaine showed increased sensitivity to bath application of 100 µM PhTx-74 compared with vehicle-treated cells, suggesting an increased contribution of GluR1-containing AMPARs to synaptic transmission after cocaine4.

    PhTx-74 was used to evaluate the effects of transmembrane AMPAR regulatory proteins (TARPs) on AMPAR conductance; 100 µM PhTx-74 blocked GluA2/A4 currents to a different degree depending on the auxiliary TARP present5.

    Target AMPA receptors
    Last update: 24/01/2020

    PhTx-74 (#P-120) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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