Catalog Number: 0961
Chemical Name: (±)-4-(4-Aminophenyl)-1,2-dihydro-1-methyl-2-propylcarbamoyl-6,7-methylenedioxyphthalazine
Biological Activity
Novel, potent, non-competitive AMPA receptor antagonist (IC50 = 2.8 μM ). Acts allosterically at the same regulatory site as GYKI 52466 and 53655 and other benzodiazepines but does not bind to the central diazepine binding site. Selective for AMPA relative to kainate receptor sub-types. Similar potency to GYKI 53655. Anticonvulsant in vivo.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in ethanol and to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold with the permission of Annovis Inc.
Background References
  1. Kainate receptor agonists, antagonists and allosteric modulators.
    Bleakman et al.
    Curr.Pharm.Des., 2002;8:873
  2. Kainate-receptor-mediated sensory synaptic transmission in mammalian spinal cord.
    Li et al.
    Nature, 1999;397:161
  3. Substituted 1,2-dihydrophthalazines: potent, selective and non-competitive inhibitors of the AMPA receptor.
    Pelletier et al.
    J.Med.Chem., 1996;39:343
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