Stereochemistry | ABSOLUTE |
Molecular Formula | C7H14NO5P |
Molecular Weight | 223.1635 |
Optical Activity | ( - ) |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)[C@H]1C[C@@H](CP(O)(O)=O)CCN1
InChI
InChIKey=LPMRCCNDNGONCD-NTSWFWBYSA-N
InChI=1S/C7H14NO5P/c9-7(10)6-3-5(1-2-8-6)4-14(11,12)13/h5-6,8H,1-4H2,(H,9,10)(H2,11,12,13)/t5-,6+/m0/s1
Molecular Formula | C7H14NO5P |
Molecular Weight | 223.1635 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Selfotel is a competitive NMDA antagonist with (-)-enantiomer is more active than ( )-enantiomer. Selfotel was investigated in phase III clinical trials for ischemic stroke and severe head injury. Development of the drug was discontinued due to lack of efficacy and possible neurotoxicity discovered in clinical trials.
CNS Activity
Originator
Approval Year
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Sourcing
PubMed
Sample Use Guides
In a clinical trial against ischemic stroke, the compound was administered intravenously at 1-2 mg/kg.
Route of Administration:
Intravenous
Activity with respect to NMDA was measured by evaluating the inhibition of NMDA-evoked release of [3H]ACh from rat striatal slices. Slices were placed in superfusion chambers and superfused with a medium containing hemicholinium-3. NMDA (50uM) was added beginning at 57 min (SI) and 93 min (SII) after superfusion was started and kept in the medium for the duration of 2 min. The antagonist was added 18 min preceding SII and kept in the medium until the end of the experiment.