Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H30N4O |
| Molecular Weight | 366.4998 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)CCNC1=NC=CC=C1C(=O)N2CCN(CC3=CC=CC=C3)CC2
InChI
InChIKey=DYTOQURYRYYNOR-UHFFFAOYSA-N
InChI=1S/C22H30N4O/c1-18(2)10-12-24-21-20(9-6-11-23-21)22(27)26-15-13-25(14-16-26)17-19-7-4-3-5-8-19/h3-9,11,18H,10,12-17H2,1-2H3,(H,23,24)
| Molecular Formula | C22H30N4O |
| Molecular Weight | 366.4998 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
NSI-189 is a novel oral drug which was developed by Neuralstem for the treatment of cognitive disorders. Now the drug is being tested in phase II of clinical trials in patients suffering from major depressive disorder. The mechanism of NSI-189 action is explained by its ability to stimulate the generation of new neurons in the hippocampus, however the exact target molecule is still unknown.
CNS Activity
Originator
Approval Year
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1144 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26643541 |
40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
NSI-189 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2791 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26643541 |
40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
NSI-189 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4384 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26643541 |
40 mg 3 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
NSI-189 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
17.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26643541 |
40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
NSI-189 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
20.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26643541 |
40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
NSI-189 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
18.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26643541 |
40 mg 3 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
NSI-189 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
40 mg 3 times / day multiple, oral Highest studied dose Dose: 40 mg, 3 times / day Route: oral Route: multiple Dose: 40 mg, 3 times / day Sources: Page: p.1377 |
unhealthy, 40.5 n = 6 Health Status: unhealthy Condition: Major depressive disorder Age Group: 40.5 Sex: M+F Population Size: 6 Sources: Page: p.1377 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| A Phase 1B, randomized, double blind, placebo controlled, multiple-dose escalation study of NSI-189 phosphate, a neurogenic compound, in depressed patients. | 2016 Oct |
|
| A Phase 1B, randomized, double blind, placebo controlled, multiple-dose escalation study of NSI-189 phosphate, a neurogenic compound, in depressed patients. | 2016 Oct |
| Substance Class |
Chemical
Created
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Edited
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| Record UNII |
YVE9U408ZL
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Validated (UNII)
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YVE9U408ZL
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NSI-189
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |
Has demonstrated the ability to stimulate neurogenesis in human hippocampal-derived neural stem cells in vitro and murine hippocampal cells in vivo.
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