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Submit ReviewL-741,626 is a potent D2 dopamine receptor selective antagonist, with affinities of 2.4, 100 and 220 nM for D2, D3 and D4 receptors respectively. Centrally active following systemic administration in vivo.
Sold with the permission of Merck Sharp and Dohme Ltd.
L-741,626 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 | 340.85 |
公式 | C20H21ClN2O |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 81226-60-0 |
PubChem ID | 133633 |
InChI Key | LLBLNMUONVVVPG-UHFFFAOYSA-N |
Smiles | OC1(CCN(CC2=CNC3=CC=CC=C23)CC1)C1=CC=C(Cl)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 | 34.09 | 100 | |
ethanol | 34.09 | 100 |
以下数据基于产品分子量 340.85。 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 | 2.93 mL | 14.67 mL | 29.34 mL |
5 mM | 0.59 mL | 2.93 mL | 5.87 mL |
10 mM | 0.29 mL | 1.47 mL | 2.93 mL |
50 mM | 0.06 mL | 0.29 mL | 0.59 mL |
参考文献是支持产品生物活性的出版物。
Bowery et al (1996) Antagonism of the effects of (+)-PD 128907 on midbrain DA neurones in rat brain slices by a selective D2 receptor antagonist L-741,626. Br.J.Pharmacol. 119 1491 PMID: 8968560
Kulagowski et al (1996) 3-[[4-(4-Chlorophenyl)piperazin-1-yl]methyl]-1H-pyrrolo[2,3-b]pyridine: an antagonist with high affinity and selectivity for the human DA D4 receptor. J.Med.Chem. 39 1941 PMID: 8642550
Millan et al (2000) S33084, a novel, potent, selective, and competitive antagonist at DA D3-receptors: II. Functional and behavioral profile compared with GR218,231 and L741,626. J.Pharmacol.Exp.Ther. 293 1063 PMID: 10869411
Pillai et al (1998) Human D2 and D4 DA receptors couple through βγ G-protein subunits to inwardly rectifying K+ channels (GIRK1) in a Xenopus oocyte expression system: selective antagonism by L-741,626 and L-745,870 respect Neuropharmacology 37 983 PMID: 9833627
If you know of a relevant reference for L-741,626, please let us know.
关键词: L-741,626, L-741,626 supplier, High, affinity, D2, antagonists, Dopamine, Receptors, dopaminergic, L741742, 1003, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 L-741,626 的部分引用包括:
Xiao et al (2017) Biased OXTergic Modulation of Midbrain DA Systems. Neuron 95 368 PMID: 28669546
Belinsky et al (2013) DA receptors in human embryonic stem cell neurodifferentiation. Stem Cells Dev 22 1522 PMID: 23286225
Lin et al (2019) Functional roles of ST8SIA3-mediated sialylation of striatal DA D2 and adenosine A2A receptors. Transl Psychiatry 9 209 PMID: 31455764
Dacks et al (2012) Olfactory modulation by DA in the context of aversive learning. J Neurophysiol 108 539 PMID: 22552185
Wang et al (2019) GPR139 and DA D2 Receptor Co-express in the Same Cells of the Brain and May Functionally Interact. Front Neurosci 13 281 PMID: 30971885
Wang et al (2015) A pivotal role of FOS-mediated BECN1/Beclin 1 upregulation in DA D2 and D3 receptor agonist-induced autophagy activation. J Neurosci 11 2057 PMID: 26649942
Billes et al (2012) Leptin reduces food intake via a DA D2 receptor-dependent mechanism. Mol Metab 1 86 PMID: 24024122
Zhang et al (2018) Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with DA Modulation. Neuron 98 918 PMID: 29754751
Newton et al (2016) Examining the Effects of Sodium Ions on the Binding of Antagonists to DA D 2 and D 3 Receptors PLoS One 11 e0158808 PMID: 27379794
Yang et al (2004) Inhibition of ATP-sensitive potassium channels by halope. Br J Pharmacol 143 960 PMID: 15533888
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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。
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