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Submit ReviewTP 003 is a GABAA receptor partial agonist that demonstrates affinity for the benzodiazepine site. Potentiates GABAA α3 response with high efficacy. Produces anxiolytic-like effects in rodent elevated plus maze via action at GABAA α2 subtype receptors. Also evokes GABAA α1 mediated sedation and GABAA α3 mediated muscle relaxation in mice.
TP 003 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 | 407.39 |
公式 | C23H16F3N3O |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 628690-75-5 |
PubChem ID | 10001434 |
InChI Key | SJMMDWXJSSJHOQ-UHFFFAOYSA-N |
Smiles | FC1=C(C(C)(O)C)C=CN2C1=NC=C2C3=CC=C(F)C(C4=CC=C(F)C=C4C#N)=C3 |
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 | 40.74 | 100 | |
ethanol | 20.37 | 50 |
以下数据基于产品分子量 407.39。 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 | 2.45 mL | 12.27 mL | 24.55 mL |
5 mM | 0.49 mL | 2.45 mL | 4.91 mL |
10 mM | 0.25 mL | 1.23 mL | 2.45 mL |
50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
参考文献是支持产品生物活性的出版物。
Dias et al (2005) Evidence for a significant role of α3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines. J.Neurosci. 25 10682 PMID: 16291941
Fischer et al (2011) Contribution of GABA(A) receptors containing α3 subunits to the therapeutic-related and side effects of benzodiazepine-type drugs in monkeys. Psychopharmacology (Berl.) 215 311 PMID: 21190016
Neumann et al (2018) TP003 is a non-selective benzodiazepine site agonist that induces anxiolysis via α2GABAA receptors. Neuropharmacology 143 71 PMID: 30240781
If you know of a relevant reference for TP 003, please let us know.
关键词: TP 003, TP 003 supplier, TP003, GABAA, GABA, receptors, a3, alpha3, α3, agonists, anxiolytic, Receptors, 4414, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 TP 003 的部分引用包括:
Seifi et al (2018) GABAA Receptor Subtypes Regulate Stress-Induced Colon Inflammation in Mice. Gastroenterology 155 852 PMID: 29802853
Soderhielm et al (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem Pharmacol 158 339 PMID: 30121248
Seifi et al (2014) Molecular and functional diversity of GABA-A receptors in the enteric nervous system of the mouse colon. Gastroenterology 34 10361 PMID: 25080596
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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 Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.