BT44 is a selective RET activator, and demonstrates the capacity to cross the blood-brain barrier, rendering it a promising candidate for the study of neurodegenerative diseases and diabetes mellitus[1].[2].
体内研究
In animal models of neuropathy, BT44 exhibits therapeutic potential. Specifically, at dosages of 5 to 25 mg/kg, administered subcutaneously every other day for durations of 10, 42, or 14 days, it mitigates sensory symptoms in both the SNL and STZ neuropathic models[1].
Furthermore, doses of 12.5 or 25 mg/kg, given subcutaneously every other day for 10 days, safeguard IB4-positive neurons within the dorsal root ganglia (DRGs) of subjects with experimental neuropathy[1].
In the context of Parkinson’s disease research, BT44, infused at 0.1 and 0.3 μg/24 hours directly into the right dorsal striatum over 14 days, counteracts amphetamine-induced motor imbalances and appears to preserve dopaminergic fibers in the striatum of the 6-OHDA rat model[2].
Moreover, with intravenous administration at 10 mg/kg, BT44 demonstrates efficient penetration through the blood-brain barrier and rapid clearance from both the circulation (half-life of 0.72 hours) and the brain (half-life of 0.47 hours) in rat models[2].
体外研究
When administered at concentrations ranging from 7.5 to 75 μM for a duration of 15 minutes, BT44 enhances RET phosphorylation and selectively initiates downstream signaling pathways in cells that express GFL receptors[1].
At doses from 0.5 to 10 μM over a period of 16 to 20 hours, BT44 fosters neurite extension from sensory neurons[1].
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