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 (4)
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.

All Tocris products are intended for laboratory research use only.

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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Safety Datasheet

References

References are publications that support the products' biological activity.

Bowery et al (1996) Antagonism of the effects of (+)-PD 128907 on midbrain dopamine 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 dopamine D4 receptor. J.Med.Chem. 39 1941 PMID: 8642550

Millan et al (2000) S33084, a novel, potent, selective, and competitive antagonist at dopamine 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 dopamine 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 r Neuropharmacology 37 983 PMID: 9833627


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4 Citations for L-741,626

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

Newton et al (2016) Examining the Effects of Sodium Ions on the Binding of Antagonists to Dopamine 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 dopamine D2 and D3 receptor agonist-induced autophagy activation. J Neurosci 11 2057 PMID: 26649942

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

Billes et al (2012) Leptin reduces food intake via a dopamine D2 receptor-dependent mechanism. Mol Metab 1 86 PMID: 24024122


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