| Stereochemistry | ABSOLUTE |
| Molecular Formula | C19H33N5O2.H2O |
| Molecular Weight | 381.5129 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.CCC(CC)COC(=O)[C@@H]1C[C@H]2C[C@@H](CCC3=NN=NN3)CC[C@H]2CN1
InChI
InChIKey=QARZUMPLLDXXBR-QKXZLCLGSA-N
InChI=1S/C19H33N5O2.H2O/c1-3-13(4-2)12-26-19(25)17-10-16-9-14(5-7-15(16)11-20-17)6-8-18-21-23-24-22-18;/h13-17,20H,3-12H2,1-2H3,(H,21,22,23,24);1H2/t14-,15+,16-,17+;/m1./s1
Tezampanel, also known as LY 293558 and NGX-424, is a drug originally developed by Eli Lilly, which is a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family. Tezampanel was in phase II clinical trial for treatment migraine, but this study was discontinued. Also this drug has several others potential pharmacological actions, one of them is anxiety disorders
CNS Activity
Approval Year
PubMed
Sample Use Guides
Single Administration of: TEZAMPANEL 40 mg; TEZAMPANEL 70 mg; TEZAMPANEL 100 mg
Route of Administration:
Other
LY293558 (Tezampanel) had a rank order of potency of GLU(K5) > or = GLU(K5/6) approximately GLU(A2i) approximately GLU(K2/5) approximately GLU(A1i) approximately GLU(A2o) approximately GLU(A3i) approximately GLU(A1o) > or = GLU(A3o) > or = GLU(A4i) approximately GLU(A4o) and >100 microM affinity for rat cortical GABA(A) receptors. Comparison of the blockade of AMPA- vs N-methyl-D-aspartate (NMDA)-induced inward currents demonstrated that LY293558 was five-fold more potent as an antagonist at AMPA vs NMDA receptors in vitro.
ACTIVE MOIETY
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
