Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C24H22N4 |
| Molecular Weight | 366.4583 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C[C@@H](C2=CC3=CC=CC=C3C=C2)C4=CC=C(C=C4C1)C5=CC=C(N)N=N5
InChI
InChIKey=VCIBGDSRPUOBOG-QFIPXVFZSA-N
InChI=1S/C24H22N4/c1-28-14-20-13-19(23-10-11-24(25)27-26-23)8-9-21(20)22(15-28)18-7-6-16-4-2-3-5-17(16)12-18/h2-13,22H,14-15H2,1H3,(H2,25,27)/t22-/m0/s1
| Molecular Formula | C24H22N4 |
| Molecular Weight | 366.4583 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Liafensine is a potential first-in-class drug targeting treatment resistant depression (TRD). Single doses of liafensine have meaningful serotonin transporter and dopamine transporter occupancy and demonstrate an acceptable safety and tolerability profile in healthy control subjects. In a number of Phase 2 clinical trials conducted by Bristol-Myers Squibb in the treatment of TRD, liafensine showed high tolerance in TRD patients but it failed to demonstrate superiority to the continuation of an existing antidepressant in patients with treatment-resistant depression.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Assessment of the Efficacy and Safety of BMS-820836 in Patients With Treatment-Resistant Major Depression: Results From 2 Randomized, Double-Blind Studies. | 2015 Aug |
|
| Safety, pharmacokinetic, and positron emission tomography evaluation of serotonin and dopamine transporter occupancy following multiple-dose administration of the triple monoamine reuptake inhibitor BMS-820836. | 2015 Feb |
|
| Comparison of different QT interval correction methods for heart rate and QT beat-to-beat method in a thorough QT study of triple monoamine reuptake inhibitor BMS-820836. | 2015 Oct |
Patents
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 01:55:52 UTC 2023
by
admin
on
Sat Dec 16 01:55:52 UTC 2023
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| Record UNII |
R34ID086Z6
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| Record Status |
Validated (UNII)
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1198790-53-2
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300000034336
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CHEMBL2364614
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DTXSID60152610
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DB14878
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9750
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58212050
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ZZ-01
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Liafensine
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R34ID086Z6
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C170121
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ACTIVE MOIETY |
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