GET73

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Chemical Structure| 202402-01-5 同义名 : -
CAS号 : 202402-01-5
货号 : A330195
分子式 : C13H16F3NO2
纯度 : 99%+
分子量 : 275.27
MDL号 : MFCD31812537
存储条件:

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 γ-Hydroxybutyrate (GHB) is a four-carbon chain monocarboxylic acid that is naturally present in the mammalian central nervous system (CNS). GET-73, a GHB analog, shows effect on hippocampal glutamate transmission. The microdialysis results indicated that local perfusion (60 min) with 10 μM – 1 μM GET73 increased extracellular glutamate levels in the CA1 region of the hippocampus of freely moving rats in a concentration dependent manner. In tissue slices from the rat hippocampus, treatment with 1 μM GET73 significantly increased K+-evoked, but not spontaneous, glutamate efflux. Moreover, 500 nM GET73 partially but significantly counteracted the increase in K+-evoked glutamate efflux induced by 100 μM CHPG, an mGluR5 agonist. These findings demonstrate that the GHB analog GET73 significantly affects glutamate transmission in the hippocampus[3]. Interestingly, the addiction of GET73 (1 and 10 µM) 1 h before and during chronic ethanol exposure prevented all the ethanol-induced effects (such as: a reduction of cell viability, an alteration of cytoskeleton, a decrease in extracellular glutamate levels and an increase of reactive oxygen species production)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.63mL

0.73mL

0.36mL

18.16mL

3.63mL

1.82mL

36.33mL

7.27mL

3.63mL

参考文献

[1]Ferraro L, Loche A, et al. The new compound GET73, N-[(4-trifluoromethyl)benzyl]4-methoxybutyramide, Regulates hippocampal Aminoacidergic transmission possibly via an allosteric modulation of mGlu5 receptor. Behavioural evidence of its

[2]Beggiato S, O'Connor WT, et al. GET73 increases rat extracellular hippocampal CA1 GABA levels through a possible involvement of local mGlu5 receptor. Synapse. 2013;67(10):678-91.

[3]Ferraro L, Beggiato S, Tomasini MC, Antonelli T, Loche A, Tanganelli S. GET73 modulates rat hippocampal glutamate transmission: evidence for a functional interaction with mGluR5. Pharmacol Rep. 2011;63(6):1359‐1371

[4]Tomasini MC, Borelli AC, Beggiato S, et al. GET73 Prevents Ethanol-Induced Neurotoxicity in Primary Cultures of Rat Hippocampal Neurons. Alcohol Alcohol. 2016;51(2):128‐135