| Stereochemistry | ACHIRAL |
| Molecular Formula | C15H16N2O |
| Molecular Weight | 240.3003 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC=CC(C)=C1NC(=O)C2=CC=C(N)C=C2
InChI
InChIKey=HZIWGOAXOBPQGY-UHFFFAOYSA-N
InChI=1S/C15H16N2O/c1-10-4-3-5-11(2)14(10)17-15(18)12-6-8-13(16)9-7-12/h3-9H,16H2,1-2H3,(H,17,18)
Ameltolide (ADD 75073, LY 201116) is a 4-aminobenzamide anticonvulsant patented by Research Corporation Technologies in the USA. Ameltolide is a sodium channel antagonist, it represents a potential therapy for the treatment of epilepsy. Ameltolide had been in phase I clinical trials by Research Corporation Technologies for the treatment of epilepsy. However, this research has been discontinued.
CNS Activity
Originator
Approval Year
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
Sourcing
PubMed
Patents
Sample Use Guides
Canine seizure model: from 2 to 15 h following a single 3 mg/kg oral ameltolide dose the mean probability of obtaining a 1 unit reduction in the seizure clinical score severity was greater than 0.80.
Route of Administration:
Oral
As a function of increasing concentration,
ameltolide produced a selective decrease
in the afterpotentials of the spontaneous
bursts before decreasing the frequency of bursts.
The concentration estimated to inhibit the number
of afterpotentials per burst by 50% (IC50 value) was
2.7 uM, whereas the ICs0 value estimated to reduce the frequency of bursts was 15 uM.
ACTIVE MOIETY
