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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- No. CAS: 80273-79-6
- Fòrmula: C22H24F4N2O
- Peso molecular:408.44
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Almacenamiento:
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
D2 Receptor 8.8 nM (IC50) |
5-HT2 Receptor 8.6 nM (IC50) |
In Vitro
Tefludazine (10 min) displays high affinity for dopamine D2 receptors in rat striatal membranes (IC50 = 8.8 nM) and 5-HT2 receptors in rat cortical membranes (IC50 = 8.6 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Tefludazine (0.22 μmol/kg; p.o.) potently antagonizes Amphetamine-induced stereotypies in male Mol/Wist rats with an ED50 of 0.22 μmol/kg and has a long duration of action of at least 24 hours[1].
Tefludazine (0.27 μmol/kg; p.o.) induces catalepsy in male Mol/Wist rats with an ED50 of 0.27 μmol/kg[1].
Tefludazine (0.0052-0.33 μmol/kg; p.o.; daily; 21 days) induces a dose-dependent decrease in spontaneously active DA neurons in both SNC and VTA[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI/BOM (male)[1]
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Dosage:0.07 μmol/kg
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Administration:i.p.
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Result:Exhibited potent neuroleptic activity, with an ED50 of 0.07 μmol/kg for antagonizing methyl phenidate-induced stereotypies.
Demonstrated a long duration of action (≥24 hours) in this model.
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Animal Model:Mol/Wist. (male)[1]
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Dosage:0.22 μmol/kg
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Administration:p.o.
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Result:Potently antagonized amphetamine-induced stereotypies, with an ED50 of 0.22 μmol/kg.
Demonstrated a long duration of action (≥ 24 hours) in this model.
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Animal Model:Mol/Wist. (male)[1]
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Dosage:0.27 μmol/kg
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Administration:p.o.
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Result:Induced catalepsy with an ED50 of 0.27 μmol/kg.
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Animal Model:Wistar rats (male, 250-300 g at study start)[2]
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Dosage:0.0052 μmol/kg; 0.010 μmol/kg; 0.020 μmol/kg; 0.083 μmol/kg; 0.33 μmol/kg
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Administration:p.o.; daily; 21 days
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Result:Exerted no effect on spontaneously active DA neurons in either SNC or VTA at 0.0052 μmol/kg.
Induced a decrease in active SNC DA neurons and a significant inhibition of active VTA DA neurons at 0.010 μmol/kg.
Caused a weak, non-significant inhibition of SNC DA neurons and a significant inhibition of VTA DA neurons at 0.020 μmol/kg.
Induced significant inhibition of SNC DA neurons and completely abolished all VTA DA neuron activity at 0.083 μmol/kg.
Induced significant inhibition of SNC DA neurons and completely abolished all VTA DA neuron activity at 0.33 μmol/kg.
Showed a statistically significant difference in the inhibitory effect on active DA neurons between SNC and VTA across all doses.
Chemical Information
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No. CAS 80273-79-6
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Peso molecular 408.44
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Fòrmula C22H24F4N2O
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SMILES
C(F)(F)(F)C=1C=C2C([C@@H](C[C@H]2N3CCN(CCO)CC3)C4=CC=C(F)C=C4)=CC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tefludazine Related Classifications
HY-184802 Related Classifications
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