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Submit Review(S)-SNAP 5114
说明： GABA uptake inhibitor
化学名： 1-[2-[tris(4-methoxyphenyl)methoxy]ethyl]-(S)-3-piperidinecarboxylic acid
纯度： ≥98% (HPLC)
生物活性 for (S)-SNAP 5114
(S)-SNAP 5114 is a GABA transport inhibitor, showing selectivity for GAT-3 and GAT-2 (IC50 values are 5, 21 and 388 μM for hGAT-3, rGAT-2 and hGAT-1 respectively). Increases thalamic GABA levels and is an anticonvulsant following systemic administration in vivo.
技术数据 for (S)-SNAP 5114
| 分子量 | 505.61 |
| 公式 | C30H35NO6 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 157604-55-2 |
| PubChem ID | 10458835 |
| InChI Key | VDLDUZLDZBVOAS-QFIPXVFZSA-N |
| Smiles | O=[C@]([C@@H]1CN(CCOC(C3=CC=C(OC)C=C3)(C4=CC=C(OC)C=C4)C2=CC=C(OC)C=C2)CCC1)O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for (S)-SNAP 5114
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| ethanol | 25.28 | 50 | |
| DMSO | 50.56 | 100 |
制备储备液 for (S)-SNAP 5114
以下数据基于产品分子量 505.61。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.98 mL | 9.89 mL | 19.78 mL |
| 5 mM | 0.4 mL | 1.98 mL | 3.96 mL |
| 10 mM | 0.2 mL | 0.99 mL | 1.98 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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产品说明书 for (S)-SNAP 5114
参考文献 for (S)-SNAP 5114
参考文献是支持产品生物活性的出版物。
Borden et al (1994) Cloning of the human homologue of the GABA transporter GAT-3 and identification of a novel inhibitor with selectivity for this site. Receptors Channels 2 207 PMID: 7874447
Borden (1996) GABA transporter heterogeneity: pharmacology and cellular localization. Neurochem.Int. 29 335 PMID: 8939442
Dalby (2000) GABA-level increasing and anticonvulsant effects of three different GABA uptake inhibitors. Neuropharmacology 39 2399 PMID: 10974324
If you know of a relevant reference for (S)-SNAP 5114, please let us know.
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关键词: (S)-SNAP 5114, (S)-SNAP 5114 supplier, GABA, reuptake, inhibitors, inhibits, BGT-1, GAT-2, GAT-3, Transporters, Monoamine, Neurotransmitter, (S)-SNAP5114, 1561, Tocris Bioscience
5 篇 (S)-SNAP 5114 的引用文献
引用文献是使用了 Tocris 产品的出版物。 (S)-SNAP 5114 的部分引用包括：
Herd et al (2013) Extrasynaptic GABA(A) receptors couple presynaptic activity to postsynaptic inhibition in the somatosensory thalamus. J Neurosci 33 14850 PMID: 24027285
Kinney (2005) GAT-3 transporters regulate inhibition in the neocortex. Mol Pain 94 4533 PMID: 16135550
Kékesi et al (2015) Recurrent seizure-like events are associated with coupled astroglial synchronization. J Neurosci 9 215 PMID: 26150770
Patel et al (2016) Context-Dependent Modulation of GABAAR-Mediated Tonic Currents. J Physiol 36 607 PMID: 26758848
Kersanté et al (2013) A functional role for both -aminobutyric acid (GABA) transporter-1 and GABA transporter-3 in the modulation of extracellular GABA and GABAergic tonic conductances in the rat hippocampus. J Neurophysiol 591 2429 PMID: 23381899
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Modulation of action potentials.
By
Sergiy Sylantyev on 12/15/2020
分析类型： In Vitro
种属： Rat
细胞系/组织： Hippocampus
(S)-SNAP 5114 was used to block a GAT-3 GABA transporter in hippocampal neural tissue. Application of (S)-SNAP 5114 decreased significantly the spiking probability in hippocampal neurons and coincidence detection time window for excitatory inputs (see illustration). 20 min. washout restored the spiking probability to ~70-80% of control value.
Preparation of 10 mM stock requires sonication.
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