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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- CAS No.: 65248-90-0
- Formule: C11H12N2
- Masse moléculaire:172.23
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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5-HT1A Receptor |
α2-adrenergic receptor |
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.
Chemical Information
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CAS No. 65248-90-0
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Masse moléculaire 172.23
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Formule C11H12N2
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SMILES
C1(/C=C/C2=CC=CC=C2)=NCCN1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tracizoline Related Classifications
HY-182597 Related Classifications
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