GsMTx4 TFA is a spider venom peptide that specifically inhibits cation-permeable mechanosensitive channels (MSCs) in the Piezo and TRP channel families. It also blocks cation-selective stretch-activated channels (SACs), reducing astrocyte toxicity and microglial reactivity induced by lysophosphatidylcholine (LPC). GsMTx4 TFA serves as a valuable pharmacological tool for exploring the role of these excitatory MSCs in both normal physiological processes and pathological conditions [1] [2] [4]
体内研究
GsMTx4 TFA (stereotactic injection, 3 μM per 1 μL, single dose) exerts neuroprotective effects by inhibiting lysophosphatidylcholine-induced astrocyte toxicity and demyelination in the cerebral cortex. [4]
GsMTx4 TFA (intraperitoneal injection, single dose of 270 μg/kg) reduces mechanical allodynia caused by inflammation and sciatic nerve injury in the Von Frey test. [6]
体外研究
In HEK293 cells transfected with Piezo1 cDNA, GsMTx4 TFA (5 μM) reduced Piezo1-mediated charge transfer to 38% of its initial level. [1]
GsMTx4 TFA (5 μM) blocks cation-selective stretch-activated channels in astrocytes, cardiomyocytes, as well as smooth and skeletal muscle cells. [2]
GsMTx4 TFA (2.5 μM, 16 hours) significantly reduces leptin-induced AMPK and MLC-2 phosphorylation in breast epithelial cells (MCF10A). [3]
GsMTx4 TFA (500 nM, 48 hours) attenuates demyelination induced by cytotoxic lipids and psychosine in organotypic cerebellar slices. [4]
GsMTx4 TFA (5 μM, 12 hours) inhibits neurogenesis and promotes astrogliogenesis in human neural stem cells. [5]
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