Ro 8-4304 hydrochloride

A Selective Antagonist of NMDA Receptors
    Cat #: R-165
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 406.88
    Purity: >98%
    Effective concentration 0.1-250 µM.
    Structure
    • Ro 8-4304 hydrochloride
    Chemical name 4-[3-[4-(4-fluorophenyl)-3,6-dihydro-2H-pyridin-1-yl]-2-hydroxypropoxy]benzamide; hydrochloride.
    Molecular formula C21H24ClFN2O3.
    CAS No.: 195988-65-9.
    PubChem CID 11957680
    Activity Ro 8-4304 is a non-competitive, state-dependent, voltage-independent NMDA receptor antagonist, highly selective for NR2B- over NR2A-containing receptors (IC50 = 0.4 μM for NR2B, >100 fold higher for NR2A, in Xenopus oocytes)1.
    References-Activity
    1. Kew, J.N. et al. (1998) Br. J. Pharmacol123, 463.
    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 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Ro 8-4304 hydrochloride
      Alomone Labs Ro 8-4304 hydrochloride inhibits NMDA receptor channels expressed in Xenopus oocytes.
      A. Time course of NR1/NR2A currents, that were elicited by transient stimulations with 100 µM glutamate and 100 µM glycine every 50 sec, while membrane potential was held at -80 mV. 250 µM Ro 8-4304 hydrochloride (#R-165), applied for 5 min (green), gradually inhibits current amplitude. B. Superimposed current traces from the recording shown in A. upon application of control (black) and of 250 µM Ro 8-4304 hydrochloride (green).
    References - Scientific background
    1. Kew, J.N. et al. (1998) Br. J. Pharmacol123, 463.
    2. Kew, J.N. et al. (1998) J. Physiol. 512, 17.
    3. Black, S.A. et al. (2014) Front. Cell Dev. Biol. 2, 45.
    Scientific background

    Ro 8-4304 hydrochloride is a non-competitive antagonist of NMDA (N-methyl-d-aspartate) receptors. Ro 8-4304 effect is a voltage-independent and demonstrates selectivity to NR2B subtype of the NMDA receptor. The compound exhibits affinity for recombinant NMDA NR2B receptors that is at least 100 fold higher than NR2A receptors1. It has an IC50 value 0.39 mM1. Ro 8-4304 acts in an ifenprodil-like (another selective inhibitor of the NMDA receptor) mechanism. It was shown to be neuroprotective in both in vitro and in vivo models of ischaemia1,2.

    NMDA receptors are heterotetrameric channels formed by the assembly of two obligatory GluN1 and two GluN2/GluN3 subunits. NMDAR plays an important role in a variety of cellular processes and brain functions such as, synaptic plasticity, addiction and stroke.

    NMDA receptors mediate physiological functions such as learning and memory formation and play a role in glutamate excitotoxicity3.

    Target NMDA receptors
    Last update: 24/01/2020

    Ro 8-4304 hydrochloride (#R-165) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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