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Submit ReviewEPPTB is a trace amine 1 (TA1) receptor antagonist/inverse agonist; exhibits a higher potency at the mouse TA1 receptor than the rat and human TA1 receptors (IC50 values are 27.5, 4539 and 7487 nM, respectively). Blocks the TA1 receptor-mediated activation of an inwardly rectifying K+ current, which increases the firing frequency of dopamine (DA) neurons in the ventral tegmental area. Increases DA potency at the D2 receptor. Also displays inverse agonism, reducing basal cAMP levels in vitro (IC50 = 19 nM).
EPPTB is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 378.39 |
公式 | C20H21F3N2O2 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 1110781-88-8 |
PubChem ID | 25175634 |
InChI Key | KLFVWQCQUXXLOU-UHFFFAOYSA-N |
Smiles | O=C(NC3=CC(OCC)=CC=C3)C1=CC(C(F)(F)F)=C(N2CCCC2)C=C1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 37.84 | 100 | |
ethanol | 37.84 | 100 |
以下数据基于产品分子量 378.39。 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 | 2.64 mL | 13.21 mL | 26.43 mL |
5 mM | 0.53 mL | 2.64 mL | 5.29 mL |
10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
参考文献是支持产品生物活性的出版物。
Bradaia et al (2009) The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in DArgic neurons of the mesolimbic system. Proc.Natl.Acad.Sci.U.S.A. 106 20081 PMID: 19892733
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关键词: EPPTB, EPPTB supplier, Parkinson's, disease, trace, amine-associated, receptors, 1, TAAR1, antagonists, dopamine, neurons, neurones, TA1, Trace, Amine, Receptor, 4518, Tocris Bioscience
平均评分: 2 (Based on 1 Review.)
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.