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Submit ReviewL-741,626
Description: High affinity D2 antagonist
Chemical Name: 3-[[4-(4-Chlorophenyl)-4-hydroxypiperidin-l-yl]methyl-1H-indole
Purity: ≥98% (HPLC)
Biological Activity for L-741,626
L-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.
Licensing Information
Sold with the permission of Merck Sharp and Dohme Ltd.
Compound Libraries for L-741,626
L-741,626 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for L-741,626
| M. Wt | 340.85 |
| Formula | C20H21ClN2O |
| Storage | Store at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for L-741,626
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.09 | 100 | |
| ethanol | 34.09 | 100 |
Preparing Stock Solutions for L-741,626
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for L-741,626
References for L-741,626
References are publications that support the biological activity of the product.
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.
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Keywords: L-741,626, L-741,626 supplier, High, affinity, D2, antagonists, Dopamine, Receptors, dopaminergic, L741742, 1003, Tocris Bioscience
10 Citations for L-741,626
Citations are publications that use Tocris products. Selected citations for L-741,626 include:
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
Do you know of a great paper that uses L-741,626 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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