Cyclotraxin B (TFA)-Get quote

Description

Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50  of  0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects[1][2][3].—Neuroscience-Neuromodulation–C50H74F3N13O19S3—-[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.|[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.|[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.—-1314.39—-O=C1N2[C@](CCC2)([H])C(N[C@H](C(NCC(N[C@H](C(N[C@@](C(N[C@H](C(N[C@H](C(NCC(N[C@@H](CSSC[C@@H](C(N[C@H]1CC(N)=O)=O)N)C(O)=O)=O)=O)CCC(O)=O)=O)CCCCN)=O)([H])[C@H](O)C)=O)CC3=CC=C(C=C3)O)=O)=O)CCSC)=O.OC(C(F)(F)F)=O–Neurological Disease–H2O–Trk Receptor–TrkB–Neuronal Signaling;Protein Tyrosine Kinase/RTK–Peptides