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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 80273-79-6
- 分子式: C22H24F4N2O
- 分子量:408.44
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
|
D2 Receptor 8.8 nM (IC50) |
5-HT2 Receptor 8.6 nM (IC50) |
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.
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.
-
Animal Model:NMRI/BOM (male)[1]
-
Dosage:0.07 μmol/kg
-
Administration:i.p.
-
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.
-
Animal Model:Mol/Wist. (male)[1]
-
Dosage:0.22 μmol/kg
-
Administration:p.o.
-
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.
-
Animal Model:Mol/Wist. (male)[1]
-
Dosage:0.27 μmol/kg
-
Administration:p.o.
-
Result:Induced catalepsy with an ED50 of 0.27 μmol/kg.
-
Animal Model:Wistar rats (male, 250-300 g at study start)[2]
-
Dosage:0.0052 μmol/kg; 0.010 μmol/kg; 0.020 μmol/kg; 0.083 μmol/kg; 0.33 μmol/kg
-
Administration:p.o.; daily; 21 days
-
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.
化学情報
-
CAS 番号 80273-79-6
-
分子量 408.44
-
分子式 C22H24F4N2O
-
SMILES
C(F)(F)(F)C=1C=C2C([C@@H](C[C@H]2N3CCN(CCO)CC3)C4=CC=C(F)C=C4)=CC1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Tefludazine 関連分類
HY-184802 関連分類
Powered by Bioz