Cyclotraxin B

Cyclotraxin B is a cyclic peptide and negative allosteric modulator of tropomysin-related kinase B (TrkB). It inhibits BDNF-induced TrkB activity in a kinase receptor activation ELISA (KIRA-ELISA) using tetracycline-responsive CHO-K1 cells expressing recombinant human TrkB (TetOn-rhTrkB cells, IC50 = 0. nM). It also inhibits BDNF-induced neurite outgrowth in nerve growth factor (NGF) non-responding mutant PC12 cells expressing TrkB (nnr5 PC12-TrkB cells, IC50 = 12. pM). Cyclotraxin B (20 mg/kg per day) reduces mechanical, but not thermal, allodynia in the ipsilateral and contralateral paw in a rat model of thermal injury exacerbated by chronic intermittent stress. Intravenous administration of cyclotraxin B fused to HIV-1 Tat protein, which increases brain delivery, increases the number of entries into and the ratio of time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity.. Solulibility: DMSO: Sparingly soluble: 1-10 mg/ml: PBS (pH 7.2): Soluble: = 10 mg/ml.