Member of the neurotrophin growth factor family that binds and activates TrkB and p75 neurotrophin receptors. Enhances the survival, growth and differentiation of neurons. BDNF expression is altered in neurodegenerative disorders such as Parkinson's and A
AZD6918 is a novel potent and selective inhibitor of the Trk tyrosine kinases. AZD-6918 attenuates the BDNF TrkB-induced protection of neuroblastoma cells from etoposide in vitro and in vivo. AZD6918 inhibited wild-type TrkB-induced cell migration and cell growth.
Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing the human transporters). Reduced haloperidol (0.5 mg kg) increases latency to paw withdrawal in mouse models of capsaicin- but not force-induced mechanical hypersensitivity.
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 p
Fabomotizole, also known as Afobazole, Obenoxazine and CM346, is an anxiolytic drug launched in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions. Its mechanism of action remains poorly defined however, with GABAergic, NGF- and BDNF-release-promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be also some involvement with serotonin receptors.