| Chemical Properties | Back Directory | [Boiling point ]
1734.8±65.0 °C(Predicted) | [density ]
1.48±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Powder | [pka]
2.95±0.70(Predicted) | [color ]
White to off-white | [Water Solubility ]
Soluble to 2 mg/ml in water |
| Hazard Information | Back Directory | [Description]
Antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic properties in mice. | [Uses]
Cyclotraxin B is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B has analgesic and anxiolytic effects[1][2][3]. | [in vivo]
Cyclotraxin B (intravenous injection; 2×200 μg; two times; with a 90-minute interval) has anxiolytic effects in mice[1].
Cyclotraxin B (intraperitoneal injection; 2×20 mg/kg; two times; with a 90-minute interval) can prevent and reverse cold allodynia induced by BDNF or infraorbital nerve ligation in mice[2]. | Animal Model: | Adult Swiss mice (20-25 g)[1] | | Dosage: | 2×200 μg (Cyclotraxin B was in the fusion form with the HIV tat protein) | | Administration: | Intravenous injection; two times with a 90-minute interval | | Result: | Dramatically decreased the total level of TrkB phosphorylation in the mouse brain.
Does not possess any antidepressant-like properties when injected acutely.
Significantly increased the time mice spent in the central area during the open field test.
Significantly increased the number of entries and the time spent in open arms by mice during the elevated-plus maze. |
| [IC 50]
TrkB | [storage]
Store at -20°C | [References]
[1] Maxime Cazorla, et al. Cyclotraxin-B, the first highly potent and selective TrkB inhibitor, has anxiolytic properties in mice. PLoS One. 2010 Mar 19;5(3):e9777. DOI:10.1371/journal.pone.0009777
[2] Luis Constandil, et al. Cyclotraxin-B, a new TrkB antagonist, and glial blockade by propentofylline, equally prevent and reverse cold allodynia induced by BDNF or partial infraorbital nerve constriction in mice. J Pain. 2012 Jun;13(6):579-89. DOI:10.1016/j.jpain.2012.03.008
[3] Michel M M Verheij, et al. Systemic Delivery of a Brain-Penetrant TrkB Antagonist Reduces Cocaine Self-Administration and Normalizes TrkB Signaling in the Nucleus Accumbens and Prefrontal Cortex. J Neurosci. 2016 Aug 3;36(31):8149-59. DOI:10.1523/JNEUROSCI.2711-14.2016 |
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BOC Sciences
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https://www.bocsci.com |
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