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说明： Potent and selective D1 antagonist
化学名： 6,7,8,9,14,15-Hexahydro-7-methyl-5H-indolo[3,2-f][3]benzazecine
纯度： ≥98% (HPLC)
生物活性 for LE 300
LE 300 is a potent and selective dopamine D1 receptor antagonist (Ki values are 0.08 - 1.9 nM and 6 - 45 nM for D1 and D2 receptors respectively). Also displays moderate affinity for the 5-HT2A receptor (Ki = 20 nM). Active in vivo.
化合物库 for LE 300
LE 300 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for LE 300
| 分子量 | 290.41 |
| 公式 | C20H22N2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 274694-98-3 |
| PubChem ID | 4350931 |
| InChI Key | YEWGIGCYIAMFMA-UHFFFAOYSA-N |
| Smiles | CN1CCC2=C(CC3=CC=CC=C3CC1)NC1=CC=CC=C21 |
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 LE 300
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| 1eq. HCl | 14.52 | 50 | |
| DMSO | 29.04 | 100 |
制备储备液 for LE 300
以下数据基于产品分子量 290.41。 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 | 3.44 mL | 17.22 mL | 34.43 mL |
| 5 mM | 0.69 mL | 3.44 mL | 6.89 mL |
| 10 mM | 0.34 mL | 1.72 mL | 3.44 mL |
| 50 mM | 0.07 mL | 0.34 mL | 0.69 mL |
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产品说明书 for LE 300
参考文献 for LE 300
参考文献是支持产品生物活性的出版物。
El-Subbagh et al (2002) DA/serotonin receptor ligands: Part IV [1]: Synthesis and pharmacology of novel 3-benzazecines and 3-benzazonines as potential 5-HT2A and DA receptor ligands. Arch.Pharm. (Weinheim). 9 443 PMID: 12447918
Kassack et al (2002) Pharmacological characterization of the benz[d]indolo[2,3-g]azecine LE300, a novel type of a nanomolar DA receptor antagonist. Naunyn Schmiedebergs Arch.Pharmacol. 366 543 PMID: 12444495
Witt et al (2000) 7-Methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine: a new heterocyclic system and a new lead compound for DA receptor antagonists. J.Med.Chem. 43 2079 PMID: 10821720
If you know of a relevant reference for LE 300, please let us know.
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关键词: LE 300, LE 300 supplier, Potent, selective, dopamine, D1, antagonists, Dopamine, Receptors, dopaminergic, LE300, and, D5, 1674, Tocris Bioscience
2 篇 LE 300 的引用文献
引用文献是使用了 Tocris 产品的出版物。 LE 300 的部分引用包括：
Cilz et al (2014) DArgic modulation of GABAergic transmission in the entorhinal cortex: concerted roles of α1 adrenoreceptors, inward rectifier K+, and T-type Ca2+ channels. Cereb Cortex 24 3195 PMID: 23843440
Gildea et al (2012) DA and angiotensin type 2 receptors cooperatively inhibit sodium transport in human renal proximal tubule cells. Hypertension 60 396 PMID: 22710646
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该领域的文献
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。
Dopamine Receptors Scientific Review
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.
Addiction Poster
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.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's Disease Poster
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.