Tracizoline
Tracizoline is an orally active I2-imidazoline receptor agonist. Tracizoline functionally modulates I2-imidazoline receptors, regulates hippocampal FADD cell fate adaptor, attenuates mechanical and thermal hyperalgesia, activates α2A-adrenergic receptors with very weak partial agonism, and induces antidepressant-like activity via 5-HT1A receptor activation. Tracizoline can be used for the research of inflammatory pain, neuropathic pain, and depression.
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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: 65248-90-0
- 分子式: C11H12N2
- 分子量:172.23
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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]
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生物活性
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化学情報
- プロトコル
- 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
IC50 & Target
[1]|
5-HT1A Receptor |
α2-adrenergic receptor |
体内実験
Tracizoline (10 mg/kg; i.p.; daily for 7 days or three doses over 24 hours) does not alter body weight, body temperature, cognitive performance, or affective-like behavior in 9-10-month-old male Sprague-Dawley rats[1].
Tracizoline (10-32 mg/kg; i.p.) produces dose-dependent antihyperalgesic effects in rats with CFA-induced inflammatory pain, reaching a maximum 62.1% MPE for mechanical hyperalgesia and 72.0% MPE for thermal hyperalgesia, with ED50 values of ~10.3 mg/kg and ~10.4 mg/kg respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 6 or 12 months old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Increased hippocampal FADD protein content by 19% compared to saline-treated control rats.
Did not significantly alter hippocampal FADD levels compared to saline-treated control rats.
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Animal Model:Sprague-Dawley (male, 9-10 months old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily for 7 days or three doses over 24 hours
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Result:Did not alter body weight over the 7-day treatment period.
Did not induce hypothermia (no significant change in core body temperature compared to controls).
Did not change the time needed to complete the 8-arm radial maze or the number of errors committed on day 1 or day 8.
Did not significantly alter the time spent immobile or climbing in the forced-swim test compared to saline-treated control rats.
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Animal Model:Sprague-Dawley (adult male, CFA-induced inflammatory pain)[2]
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Dosage:3.2 mg/kg; 10 mg/kg; 32 mg/kg
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Administration:i.p.
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Result:Increased paw withdrawal threshold (mechanical hyperalgesia) and paw withdrawal latency (thermal hyperalgesia) dose-dependently in the CFA-treated paw, with no effect on the non-injured paw.
Significantly increased both paw withdrawal threshold and paw withdrawal latency in the CFA-treated paw at 10 mg/kg and 32 mg/kg (P < 0.05).
Produced a maximum of 62.1% maximal possible effect (MPE) in the von Frey test (mechanical hyperalgesia) and 72.0% MPE in the plantar test (thermal hyperalgesia).
Reached ED50 values of 10 mg/kg in the von Frey test and 10 mg/kg in the plantar test.
化学情報
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CAS 番号 65248-90-0
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分子量 172.23
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分子式 C11H12N2
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SMILES
C1(/C=C/C2=CC=CC=C2)=NCCN1
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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.
プロトコル
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
純度とドキュメンテーション
参考文献
[1]. Hernández-Hernández E, et al. Evaluating the effects of 2-BFI and tracizoline, two potent I2-imidazoline receptor agonists, on cognitive performance and affect in middle-aged rats. Naunyn Schmiedebergs Arch Pharmacol. 2021;394(5):989-996. [Content Brief]
[2]. Li JX, et al. Antihyperalgesic effects of imidazoline I(2) receptor ligands in rat models of inflammatory and neuropathic pain. Br J Pharmacol. 2014;171(6):1580-1590. [Content Brief]
[3]. Del Bello F, et al. The Versatile 2-Substituted Imidazoline Nucleus as a Structural Motif of Ligands Directed to the Serotonin 5-HT1A Receptor. ChemMedChem. 2016;11(20):2287-2298. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Tracizoline 関連分類
HY-182597 関連分類
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