SAK 3 是一种有效的 T 型电压门控 Ca2+ 通道 (T-VGCCs) 增强剂。
Potent CaV3.1 and CaV3.3 activator. Enhances CaV3.1 and CaV3.3, but not CaV3.2 activity at concentrations of 0.01 - 10 M in neuro2A cells in vitro. Elevates ACh levels in hippocampus. Rescues impaired memory-related behaviors, promotes adult neurogenesis and displays antidepressant-like effects in OBX mice. Orally bioavailable.
Yabuki et al (2017) Pharmacological properties of SAK3, a novel T-type voltage-gated Ca2+ channel enhancer. Neuropharmacology 117 1 PMID:28093211 |Xu et al (2018) T-type calcium channel enhancer SAK3 produces anti-depressant-like effects by promoting adult hippocampal neurogenesis in olfactory bulbectomized mice. J.Pharmacol.Sci. 137 333 PMID:30196018
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