Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C20H19ClFNO4 |
Molecular Weight | 391.821 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(=O)C1=CC2=C(OC(C)(C)[C@@H](O)[C@H]2NC(=O)C3=CC=C(F)C(Cl)=C3)C=C1
InChI
InChIKey=XLIIRNOPGJTBJD-ROUUACIJSA-N
InChI=1S/C20H19ClFNO4/c1-10(24)11-5-7-16-13(8-11)17(18(25)20(2,3)27-16)23-19(26)12-4-6-15(22)14(21)9-12/h4-9,17-18,25H,1-3H3,(H,23,26)/t17-,18-/m0/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/10021946Curator's Comment: description was created on several sources, including https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3142555/
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10021946
Curator's Comment: description was created on several sources, including https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3142555/
Tonabersat is a unique compound with demonstrated activity as a gap-junction inhibitor in animal studies. In preclinical and clinical trials, tonabersat was well tolerated, with no cardiovascular effects; the pharmacokinetic profile suggested its usefulness in the prophylaxis of migraine. The basis of its high efficacy is inhibiting neuronal hyperexcitability and trigeminal nerve stimulated neurogenic inflammation in rodent models. Tonabersat inhibits the CSD (cortical spreading depression) that is believed to underlie the aura of migraine.
CNS Activity
Originator
Approval Year
Doses
Dose | Population | Adverse events |
---|---|---|
80 mg single, oral (unknown) Highest studied dose |
unhealthy n = 109 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 109 Sources: |
Other AEs: Dizziness, Nausea... Other AEs: Dizziness (5.5%) Sources: Nausea (4.6%) Vertigo (4.6%) Somnolence (0.9%) Abdominal pain (0.9%) |
40 mg 1 times / day multiple, oral (total daily dose) Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy n = 58 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 58 Sources: |
Disc. AE: dizziness, nausea... AEs leading to discontinuation/dose reduction: dizziness (1 pt) Sources: nausea (2 patients) nausea (1 pt) Drowsiness (severe, 1 pt) headache (1 pt) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Abdominal pain | 0.9% | 80 mg single, oral (unknown) Highest studied dose |
unhealthy n = 109 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 109 Sources: |
Somnolence | 0.9% | 80 mg single, oral (unknown) Highest studied dose |
unhealthy n = 109 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 109 Sources: |
Nausea | 4.6% | 80 mg single, oral (unknown) Highest studied dose |
unhealthy n = 109 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 109 Sources: |
Vertigo | 4.6% | 80 mg single, oral (unknown) Highest studied dose |
unhealthy n = 109 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 109 Sources: |
Dizziness | 5.5% | 80 mg single, oral (unknown) Highest studied dose |
unhealthy n = 109 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 109 Sources: |
dizziness | 1 pt Disc. AE |
40 mg 1 times / day multiple, oral (total daily dose) Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy n = 58 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 58 Sources: |
headache | 1 pt Disc. AE |
40 mg 1 times / day multiple, oral (total daily dose) Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy n = 58 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 58 Sources: |
nausea | 1 pt Disc. AE |
40 mg 1 times / day multiple, oral (total daily dose) Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy n = 58 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 58 Sources: |
nausea | 2 patients Disc. AE |
40 mg 1 times / day multiple, oral (total daily dose) Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy n = 58 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 58 Sources: |
Drowsiness | severe, 1 pt Disc. AE |
40 mg 1 times / day multiple, oral (total daily dose) Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy n = 58 Health Status: unhealthy Condition: migraine Sex: M+F Food Status: UNKNOWN Population Size: 58 Sources: |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT00311662
Take 40 mg daily for 12 weeks.
Route of Administration:
Oral
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NCI_THESAURUS |
C264
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ACTIVE MOIETY