Tracazolate
Tracazolate (ICI 136753) is an orally active non-benzodiazepine anxiolytic. Tracazolate significantly enhances the binding of the radioligand 3H-flunitrazepam (3H-FLU) to brain tissue benzodiazepine receptors. Tracazolate enhances the binding of γ-aminobutyric acid (GABA) to its receptors. Tracazolate exhibits anticonvulsant activity. Tracazolate can be used in anxiety-related research.
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- CAS 番号: 41094-88-6
- 分子式: C16H24N4O2
- 分子量:304.39
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | Inhibition |
22.52 %
Compound: TRACAZOLATE
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Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
10.21203/rs.3.rs-23951/v1 |
体外実験
Tracazolate enhances the binding of [3H]flunitrazepam to benzodiazepine receptor sites in mammalian brain tissue[1].
Tracazolate enhances the binding of [3H]GABA to its receptor sites in mammalian brain tissue[1].
Tracazolate enhances the binding of [3H]flunitrazepam to brain tissue[2].
Tracazolate enhances GABA binding to rat brain membrane fractions[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
At all tested doses, Tracazolate (5-40 mg/kg; i.p.; p.o.; single administration) produces no statistically significant anxiolytic activity in the rat Geller conflict test[1].
Tracazolate (40-80 mg/kg; p.o.; once daily; for 12 consecutive days) shows no tolerance to its anxiolytic activity after intragastric administration at 40 or 80 mg/kg once daily for 12 consecutive days in rats[1].
Tracazolate (25-200 mg/kg; oral administration; single dose) exhibits dose-dependent anxiolytic activity in the mouse exploratory conflict test, with a minimum effective dose of 25 mg/kg p.o[1].
Tracazolate (i.p.; single administration) acts as a weak antagonist against Metrazol- and Bicuculline (HY-N0219)-induced convulsions in mice, with an i.p. ED50 of 27.7 mg/kg and 22.5 mg/kg, respectively[1].
Tracazolate (oral administration; single dose) impairs the rotarod performance of mice at high doses, with an oral ED50 of 117.1 mg/kg[1]
Tracazolate (oral administration; single dose) does not impair rotarod performance in rats when administered at doses up to 400 mg/kg via intragastric gavage[1].
Tracazolate (12.5-100 mg/kg; p.o.; single administration) does not significantly exacerbate ethanol-induced impairment in the rotarod test in mice, even at an intragastric dose as high as 100 mg/kg[1].
Tracazolate (12.5-50 mg/kg; p.o.; single administration) enhances ethanol-induced sleep duration in mice at oral doses of 25 mg/kg and above, and its minimum effective dose is comparable to that for anxiolytic effects[1].
Tracazolate (5-10 mg/kg; p.o.; single administration) potentiates the anxiolytic activity of Chlordiazepoxide in a rat model of shock-induced feeding inhibition[1].
Tracazolate (12.5 mg/kg; intraperitoneal injection; single administration) enhances the anticonvulsant activity of chlordiazepoxide in mice, reducing the ED50 of Chlordiazepoxide by approximately 6-fold[1].
Tracazolate (20-40 mg/kg; i.p.; single administration) does not increase water intake in non-water-deprived rats, nor does it do so at i.p. doses of 20 or 40 mg/kg, indicating that its anxiolytic activity is independent of drive[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 180-220 g)[1]
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Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg; 80 mg/kg
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Administration:i.p.; p.o.; single dose
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Result:Produced a statistically significant dose-dependent increase in mean number of shocks taken.
Had a relative potency of 1/4 to 1/2 that of chlordiazepoxide.
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Animal Model:Sprague-Dawley (male, 240-260 g, maintained at ~80% free-feeding weight)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:i.p.; p.o.; single dose
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Result:Produced non-significant increases in punished responding of +7.7% (5 mg/kg i.p.), +2.1% (10 mg/kg i.p.), and +29.0% (20 mg/kg i.p.).
Produced a +126.6% increase in punished responding at 40 mg/kg p.o. that did not reach statistical significance.
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Animal Model:Wistar (male, 180-220 g)[1]
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Dosage:40 mg/kg; 80 mg/kg
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Administration:p.o.; daily; 12 days
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Result:Retained statistically significant anxiolytic activity, with mean shocks taken of 9.95 (40 mg/kg) and 10.16 (80 mg/kg).
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Animal Model:Swiss-Webster (male, 18-25 g)[1]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg; 200 mg/kg
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Administration:p.o.; single dose
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Result:Reached a minimal effective dose (MED) of 25 mg/kg p.o., which produced a statistically significant increase in mean number of shocks taken.
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Animal Model:Swiss-Webster (male, 18-25 g)[1]
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Dosage:ED50 27.7 mg/kg (95% confidence limits 19.4-38.4)
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Administration:i.p.; single dose
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Result:Had an ED50 of 27.7 mg/kg i.p. (95% confidence limits 19.4-38.4) for protection against metrazol-induced convulsions.
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Animal Model:Swiss-Webster (male, 18-25 g)[1]
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Dosage:ED50 22.5 mg/kg (95% confidence limits 8.9-51.9)
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Administration:i.p.; single dose
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Result:Had an ED50 of 22.5 mg/kg i.p. (95% confidence limits 8.9-51.9) for protection against bicuculline-induced convulsions.
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Animal Model:Swiss-Webster (male, 18-25 g)[1]
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Dosage:ED50 117.1 mg/kg (95% confidence limits 85.0-191.1)
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Administration:p.o.; single dose
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Result:Had an ED50 of 117.1 mg/kg p.o. (95% confidence limits 85.0-191.1) for impairment of rotorod performance.
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Animal Model:Wistar (male, 180-220 g)[1]
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Dosage:400 mg/kg
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Administration:p.o.; single dose
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Result:Failed to significantly impair rotorod performance at the highest tested dose of 400 mg/kg p.o.
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Animal Model:Swiss-Webster (male, 18-25 g)[1]
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Dosage:12.5 mg/kg; 25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; single dose
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Result:Did not significantly enhance ethanol-induced rotorod impairment; ataxia rates were 0.0%, 0.0%, 16.7%, and 16.7% respectively.
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Animal Model:Swiss-Webster (male, 18-25 g)[1]
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Dosage:12.5 mg/kg; 25 mg/kg; 50 mg/kg
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Administration:p.o.; single dose
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Result:Reached a minimal effective dose of 25 mg/kg p.o., which produced a statistically significant prolongation of ethanol-induced sleeptime to 59.9 minutes.
Prolonged sleeptime to 95.0 minutes at 50 mg/kg p.o.
Had no significant effect at 12.5 mg/kg p.o.
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Animal Model:Wistar (male, 180-220 g)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:p.o.
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Result:Produced statistically significant increases in mean number of shocks taken when combined with chlordiazepoxide 2.5 mg/kg p.o. (a sub-effective dose alone), with a potentiative effect greater than the sum of individual drug effects.
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Animal Model:Swiss-Webster (male, 18-25 g)[1]
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Dosage:12.5 mg/kg
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Administration:i.p.
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Result:Reduced the ED50 of chlordiazepoxide for protection against metrazol-induced convulsions from 4.9 mg/kg p.o. to 0.8 mg/kg p.o., making chlordiazepoxide approximately 6 times more potent.
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Animal Model:Wistar (male, 180-220 g)[1]
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Dosage:20 mg/kg; 40 mg/kg
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Administration:i.p.
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Result:Did not enhance water consumption; mean lick counts were 246.5 and 222.14 respectively, which were not significantly different from controls.
化学情報
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CAS 番号 41094-88-6
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分子量 304.39
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分子式 C16H24N4O2
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SMILES
O=C(OCC)C1=C(N=C2C(C=NN2CC)=C1NCCCC)C
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別名
ICI 136753
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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]. Patel JB, et al. Pharmacological properties of tracazolate: a new non-benzodiazepine anxiolytic agent. Eur J Pharmacol. 1982;78(3):323-333. [Content Brief]
[2]. Patel JB, et al. Preclinical studies with pyrazolopyridine non-benzodiazepine anxiolytics: ICI 190,622. Pharmacol Biochem Behav. 1988;29(4):775-779. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Tracazolate 関連分類
HY-B1803 関連分類
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