EMD 281014 hydrochloride

Pricing Availability   Qty
说明: Selective 5-HT2A antagonist
化学名: 7-[[4-[2-(4-Fluorophenyl)ethyl]-1-piperazinyl]carbonyl]-1H-indole-3-carbonitrile hydrochloride
纯度: ≥98% (HPLC)
说明书
引用文献 (2)
评论
文献 (3)

生物活性 for EMD 281014 hydrochloride

EMD 281014 hydrochloride is a selective 5-HT2A antagonist; displays high affinity for human 5-HT2A over 5-HT2C receptors (Ki values are 0.87 and 557 nM respectively). Exhibits low off-target activity (Ki values are >1000 and 1268 nM for human D2 receptors and IKr channels, respectively).

技术数据 for EMD 281014 hydrochloride

分子量 412.89
公式 C22H21FN4O.HCl
储存 Desiccate at RT
纯度 ≥98% (HPLC)
CAS Number 443144-27-2
PubChem ID 9887933
InChI Key UYGNZRVLPYZLTF-UHFFFAOYSA-N
Smiles O=C(N3CCN(CCC4=CC=C(F)C=C4)CC3)C1=C2C(C(C#N)=CN2)=CC=C1.Cl

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 EMD 281014 hydrochloride

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 41.29 100
ethanol 10.32 25

制备储备液 for EMD 281014 hydrochloride

以下数据基于产品分子量 412.89。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.42 mL 12.11 mL 24.22 mL
5 mM 0.48 mL 2.42 mL 4.84 mL
10 mM 0.24 mL 1.21 mL 2.42 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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产品说明书 for EMD 281014 hydrochloride

参考文献 for EMD 281014 hydrochloride

参考文献是支持产品生物活性的出版物。

Ladduwahetty et al (2006) A new class of selective, non-basic 5-HT2A receptor antagonists. Bioorg.Med.Chem.Lett. 16 3201 PMID: 16632354

Patel et al (2004) The highly selective 5-hydroxytryptamine (5-HT)2A receptor antagonist, EMD 281014, significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test. Synapse 52 73 PMID: 14755634

Bartoszyk et al (2003) EMD 281014, a new selective serotonin 5-HT2A receptor antagonist. Eur.J.Pharmacol. 473 229 PMID: 12892843

Hamadjida et al (2018) The highly selective 5-HT2A antagonist EMD-281,014 reduces dyskinesia and psychosis in the l-DOPA-treated parkinsonian marmoset. Neuropharmacology. 139 61 PMID: 29969592


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关键词: EMD 281014 hydrochloride, EMD 281014 hydrochloride supplier, EMD281014, 5-HT2A, selective, serotonergics, antagonists, h5-HT2A, h5-HT2C, Receptors, 4470, Tocris Bioscience

2 篇 EMD 281014 hydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 EMD 281014 hydrochloride 的部分引用包括:

Georgia et al (2019) Multimodal Single-Cell Analysis Reveals Physiological Maturation in the Developing Human Neocortex. Neuron 102 143-158.e7 PMID: 30770253

Wieland B et al (2020) Serotonin Receptor 2A Activation Promotes Evolutionarily Relevant Basal Progenitor Proliferation in the Developing Neocortex. Neuron 108 1113-1129.e6 PMID: 33080227


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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!

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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.

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