Tracazolate free base
Tracazolate (ICI 136753) is an orally active non-benzodiazepine anxiolytic.
For research use only. Not for human or veterinary use.
Tracazolate structure
CAS No.: 41094-88-6
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 10 mg | USD 340.00 | BP-02206-10mg | In stock | Get quote |
| 25 mg | USD 650.00 | BP-02206-25mg | In stock | Get quote |
| 50 mg | USD 1,040.00 | BP-02206-50mg | In stock | Get quote |
| 100 mg | USD 1,660.00 | BP-02206-100mg | In stock | Get quote |
| 250 mg | USD 3,300.00 | BP-02206-250mg | In stock | Get quote |
| 500 mg | Inquire | BP-02206-500mg | In stock | Inquire |
| 1 g | Inquire | BP-02206-1g | In stock | Inquire |
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Description
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].
Biological activity
In Vitro Tracazolate enhances the binding of [3H]flunitrazepam to benzodiazepine receptor sites in mammalian brain tissue. Tracazolate enhances the binding of [3H]GABA to its receptor sites in mammalian brain tissue. Tracazolate enhances the binding of [3H]flunitrazepam to brain tissue. Tracazolate enhances GABA binding to rat brain membrane fractions. In Vivo Tracazolate (10-80 mg/kg; i.p.; p.o.; single administration) exhibits dose-dependent anxiolytic activity in rat shock-induced drinking suppression tests, with a relative potency of 1/4 to 1/2 that of Chlordiazepoxide. 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. 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. 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. 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. Tracazolate (oral administration; single dose) impairs the rotarod performance of mice at high doses, with an oral ED50 of 117.1 mg/kg Tracazolate (oral administration; single dose) does not impair rotarod performance in rats when administered at doses up to 400 mg/kg via intragastric gavage. 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. 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. Tracazolate (5-10 mg/kg; p.o.; single administration) potentiates the anxiolytic activity of Chlordiazepoxide in a rat model of shock-induced feeding inhibition. 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. 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.
Identifiers
- SMILES
-
O=C(OCC)C1=C(N=C2C(C=NN2CC)=C1NCCCC)C - InChIKey
-
PCTRYMLLRKWXGF-UHFFFAOYSA-N
Specifications
- MW (average)
- 304.3874
- Formula
- C16H24N4O2
- CAS No.
- 41094-88-6
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Please store the product under the recommended conditions in the Certificate of Analysis.