L-741,626

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Cat.No. 1003 - L-741,626 | C20H21ClN2O | CAS No. 81226-60-0
Description: High affinity D2 antagonist
Chemical Name: 3-[[4-(4-Chlorophenyl)-4-hydroxypiperidin-l-yl]methyl-1H-indole
Purity: ≥98% (HPLC)
Datasheet
Citations (6)
Reviews
Literature

Biological Activity

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.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 34.09 100
ethanol 34.09 100

Preparing Stock Solutions

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

Certificate of Analysis / Product Datasheet
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References

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


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Keywords: L-741,626, L-741,626 supplier, High, affinity, D2, antagonists, Dopamine, Receptors, dopaminergic, L741742, 1003, Tocris Bioscience

6 Citations for L-741,626

Citations are publications that use Tocris products. Selected citations for L-741,626 include:

Belinsky et al (2013) DA receptors in human embryonic stem cell neurodifferentiation. Stem Cells Dev 22 1522 PMID: 23286225

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

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

Dacks et al (2012) Olfactory modulation by DA in the context of aversive learning. J Neurophysiol 108 539 PMID: 22552185

Yang et al (2004) Inhibition of ATP-sensitive potassium channels by haloperidol. Br J Pharmacol 143 960 PMID: 15533888


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