GPI-1046 是一种不含抗生素作用的免疫亲和素配体,通过上调 PFC 和 NAc 核心中的谷氨酸转运蛋白1 (GLT1) 来减少乙醇摄入。GPI-1046 是 FK506 的类似物,在神经退行性疾病模型中显示出神经保护作用。GPI-1046 易穿过血脑屏障并促进中枢神经系统中多巴胺 (DA) 细胞的再生,这与啮齿动物模型中的功能恢复相关。
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GPI-1046 is a immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models[1]. GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models[2].
[1]. Sari Y, et al. Neuroimmunophilin GPI-1046 reduces ethanol consumption in part through activation of GLT1 in alcohol-preferring rats. Neuroscience. 2012 Dec 27;227:327-35. [2]. Eberling JL, et al. The immunophilin ligand GPI-1046 does not have neuroregenerative effects in MPTP-treated monkeys. Exp Neurol. 2002 Dec;178(2):236-42.
FFN-102 (trifluoroacetate salt)
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