Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C22H24F4N2O |
| Molecular Weight | 408.4324 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OCCN1CCN(CC1)[C@@H]2C[C@H](C3=C2C=C(C=C3)C(F)(F)F)C4=CC=C(F)C=C4
InChI
InChIKey=JSBWGXQXCRYYTG-PZJWPPBQSA-N
InChI=1S/C22H24F4N2O/c23-17-4-1-15(2-5-17)19-14-21(28-9-7-27(8-10-28)11-12-29)20-13-16(22(24,25)26)3-6-18(19)20/h1-6,13,19,21,29H,7-12,14H2/t19-,21+/m0/s1
Tefludazine (Lu 18-012) is a mixed D2 and 5-HT2 receptor antagonist that was developed as a potential antipsychotic compound. It was shown that tefludazine induced a dose-dependent decrease in both nigra pars compacta (SNC) and ventral tegmental area (VTA) dopamine (DA) activity. The development of the drug was discontinued in Phase I due to toxicological findings in dogs.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans. | 1983 Jul |
|
| Differential effects after repeated treatment with haloperidol, clozapine, thioridazine and tefludazine on SNC and VTA dopamine neurones in rats. | 1988 |
|
| Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity. | 1988 Dec |
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Code | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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NCI_THESAURUS |
C66883
Created by
admin on Sat Dec 16 16:53:39 UTC 2023 , Edited by admin on Sat Dec 16 16:53:39 UTC 2023
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NCI_THESAURUS |
C66885
Created by
admin on Sat Dec 16 16:53:39 UTC 2023 , Edited by admin on Sat Dec 16 16:53:39 UTC 2023
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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100000082459
Created by
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PRIMARY | |||
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SUB10867MIG
Created by
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80273-79-6
Created by
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CHEMBL95636
Created by
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PRIMARY | |||
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C054810
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80680-06-4
Created by
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SUPERSEDED | |||
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71240
Created by
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PRIMARY | |||
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DTXSID20878607
Created by
admin on Sat Dec 16 16:53:39 UTC 2023 , Edited by admin on Sat Dec 16 16:53:39 UTC 2023
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PRIMARY | |||
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C90626
Created by
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PRIMARY | |||
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2XUS19W8FE
Created by
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PRIMARY | |||
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5227
Created by
admin on Sat Dec 16 16:53:39 UTC 2023 , Edited by admin on Sat Dec 16 16:53:39 UTC 2023
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PRIMARY |
ACTIVE MOIETY
