80273-79-6
Chemical Structure
Tefludazine
- CAS No.: 80273-79-6
- Formula:C22H24F4N2O
- Molecular Weight:408.44
IUPAC Name: 2-(4-((1R,3S)-3-(4-fluorophenyl)-6-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl)piperazin-1-yl)ethan-1-ol
InChIKey: JSBWGXQXCRYYTG-PZJWPPBQSA-N
SMILES: C(F)(F)(F)C=1C=C2C([C@@H](C[C@H]2N3CCN(CCO)CC3)C4=CC=C(F)C=C4)=CC1
Biological Activity: Tefludazine is an orally active antagonist of dopamine D2 receptor with an IC50 of 8.8 nM and 5-HT2 receptor with an IC50 of 8.6 nM. Tefludazine moderately inhibits the uptake of dopamine, norepinephrine and serotonin in rat brain synaptosomes, with IC50 values of 520 nM, 660 nM and 7000 nM, respectively. Tefludazine exhibits long-acting antipsychotic activity, lacks anticholinergic activity, shows Clozapine (HY-14539)-like effects at low doses and Haloperidol (HY-14538)-like effects at high doses. Tefludazine can be used for the research of psychotic disorders[1][2].
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Tefludazine | Tefludazine is an orally active antagonist of dopamine D2 receptor with an IC50 of 8.8 nM and 5-HT2 receptor with an IC50 of 8.6 nM. Tefludazine moderately inhibits the uptake of dopamine, norepinephrine and serotonin in rat brain synaptosomes, with IC50 values of 520 nM, 660 nM and 7000 nM, respectively. Tefludazine exhibits long-acting antipsychotic activity, lacks anticholinergic activity, shows Clozapine (HY-14539)-like effects at low doses and Haloperidol (HY-14538)-like effects at high doses. Tefludazine can be used for the research of psychotic disorders. | |||||||||||||||||||||
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- [1]. Bøgesø KP, et al. Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans. Journal of medicinal chemistry. 1983 Jul;26(7):935-47. [Content Brief]
- [2]. Skarsfeldt T, et al. Differential effects after repeated treatment with haloperidol, clozapine, thioridazine and tefludazine on SNC and VTA dopamine neurones in rats. Life sciences. 1988;42(10):1037-44. [Content Brief]
Keywords
