2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Tracazolate

Tracazolate (ICI 136753) 是一种具有口服活性的非苯二氮䓬类抗焦虑剂。Tracazolate Tracazolate能显著增强放射性配体 ³H-氟硝西泮 (³H-FLU) 与脑组织苯二氮䓬受体的结合。Tracazolate 能增强 γ-氨基丁酸 (GABA) 与其受体的结合。Tracazolate 具有抗惊厥活性。Tracazolate 可用于焦虑相关研究。

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Tracazolate

Tracazolate Chemical Structure

CAS No. : 41094-88-6

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Tracazolate 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2].

体外研究
(In Vitro)

Tracazolate 可增强 [3H]flunitrazepam 与哺乳动物脑组织中苯二氮䓬受体位点的结合[1]。
Tracazolate 可增强 [3H]GABA 与哺乳动物脑组织中其受体位点的结合[1]。
Tracazolate 可增强 [3H]flunitrazepam 与脑组织的结合作用[2]。
Tracazolate 可增强 GABA 与大鼠脑细胞膜组分的结合作用[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Tracazolate 相关抗体:
体内研究
(In Vivo)

Tracazolate (10-80 mg/kg；腹腔注射；口服；单次给药) 在大鼠休克诱导的饮水抑制试验中呈现剂量依赖性的抗焦虑活性，相对效力为 Chlordiazepoxide的 1/4 至 1/2[1]。
Tracazolate (5-40 mg/kg；腹腔注射；口服；单次给药) 在大鼠 Geller 冲突试验中，各受试剂量均未产生具有统计学意义的抗焦虑活性[1]。
Tracazolate (40-80 mg/kg；口服；每日 1 次；连续 12 天) 在大鼠中连续 12 天每日灌胃给予 40 或 80 mg/kg 后，其抗焦虑活性未出现耐受现象[1]。
Tracazolate (25-200 mg/kg；口服；单次给药) 在小鼠探索冲突试验中表现出剂量依赖性的抗焦虑活性，最小有效剂量为 25 mg/kg p.o[1]。
Tracazolate (腹腔注射；单次给药) 可作为小鼠中 Metrazol 和 Bicuculline (HY-N0219) 诱导惊厥的弱拮抗剂，其腹腔注射 ED50 分别为 27.7 和 22.5 mg/kg[1]。
Tracazolate (口服；单次给药) 在高剂量下会损害小鼠的转棒表现，其经口给药的 ED50 为 117.1 mg/kg[1]
Tracazolate (口服；单次给药) 在大鼠中给药剂量高达 400 mg/kg 灌胃时，不会损害转棒表现[1]。
Tracazolate (12.5-100 mg/kg；口服；单次给药) 在小鼠中，当灌胃剂量高达 100 mg/kg 时，不会显著加重乙醇诱导的转棒实验损伤[1]。
Tracazolate (12.5-50 mg/kg；口服；单次给药) 在 25 mg/kg 及以上的口服剂量下可增强小鼠中乙醇诱导的睡眠时间，其最低有效剂量与抗焦虑作用的最低有效剂量相当[1]。
Tracazolate (5-10 mg/kg；口服；单次给药) 在大鼠休克诱导的摄食抑制实验中可增强 Chlordiazepoxide 的抗焦虑活性[1]。
Tracazolate (12.5 mg/kg；腹腔注射；单次给药) 可增强氯氮䓬在小鼠体内的抗惊厥活性，使 Chlordiazepoxide 的 ED50 降低约 6 倍[1]。
Tracazolate (20-40 mg/kg；腹腔注射；单次给药) 不会增加非禁水大鼠的饮水量，其腹腔注射剂量为 20 或 40 mg/kg 时亦是如此，表明其抗焦虑活性与驱力无关[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar (male, 180-220 g)[1]
Dosage: 10 mg/kg; 20 mg/kg; 40 mg/kg; 80 mg/kg
Administration: i.p.; p.o.; single dose
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.
Animal Model: Sprague-Dawley (male, 240-260 g, maintained at ~80% free-feeding weight)[1]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: i.p.; p.o.; single dose
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.
Animal Model: Wistar (male, 180-220 g)[1]
Dosage: 40 mg/kg; 80 mg/kg
Administration: p.o.; daily; 12 days
Result: Retained statistically significant anxiolytic activity, with mean shocks taken of 9.95 (40 mg/kg) and 10.16 (80 mg/kg).
Animal Model: Swiss-Webster (male, 18-25 g)[1]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg; 200 mg/kg
Administration: p.o.; single dose
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.
Animal Model: Swiss-Webster (male, 18-25 g)[1]
Dosage: ED50 27.7 mg/kg (95% confidence limits 19.4-38.4)
Administration: i.p.; single dose
Result: Had an ED50 of 27.7 mg/kg i.p.
(95% confidence limits 19.4-38.4) for protection against metrazol-induced convulsions.
Animal Model: Swiss-Webster (male, 18-25 g)[1]
Dosage: ED50 22.5 mg/kg (95% confidence limits 8.9-51.9)
Administration: i.p.; single dose
Result: Had an ED50 of 22.5 mg/kg i.p.
(95% confidence limits 8.9-51.9) for protection against bicuculline-induced convulsions.
Animal Model: Swiss-Webster (male, 18-25 g)[1]
Dosage: ED50 117.1 mg/kg (95% confidence limits 85.0-191.1)
Administration: p.o.; single dose
Result: Had an ED50 of 117.1 mg/kg p.o.
(95% confidence limits 85.0-191.1) for impairment of rotorod performance.
Animal Model: Wistar (male, 180-220 g)[1]
Dosage: 400 mg/kg
Administration: p.o.; single dose
Result: Failed to significantly impair rotorod performance at the highest tested dose of 400 mg/kg p.o.
Animal Model: Swiss-Webster (male, 18-25 g)[1]
Dosage: 12.5 mg/kg; 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: p.o.; single dose
Result: Did not significantly enhance ethanol-induced rotorod impairment; ataxia rates were 0.0%, 0.0%, 16.7%, and 16.7% respectively.
Animal Model: Swiss-Webster (male, 18-25 g)[1]
Dosage: 12.5 mg/kg; 25 mg/kg; 50 mg/kg
Administration: p.o.; single dose
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.
Animal Model: Wistar (male, 180-220 g)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: p.o.
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.
Animal Model: Swiss-Webster (male, 18-25 g)[1]
Dosage: 12.5 mg/kg
Administration: i.p.
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.
Animal Model: Wistar (male, 180-220 g)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: i.p.
Result: Did not enhance water consumption; mean lick counts were 246.5 and 222.14 respectively, which were not significantly different from controls.
分子量

304.39

Formula

C16H24N4O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Tracazolate 相关分类

  • 摩尔计算器

  • 稀释计算器

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Keywords:

Tracazolate41094-88-6ICI 136753ICI136753ICI-136753GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorconvulsionsrat brain membrane fractionsratsGeller Conflict testmiceShock-induced Suppression of Drinking testanxietyGABA receptorsbenzodiazepine receptorsmammalian brain tissueInhibitorinhibitorinhibit

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