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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.
Sold with the permission of Merck Sharp and Dohme Ltd.
Compound Libraries for L-741,626
Technical Data for L-741,626
|Storage||Store at RT|
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|
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|
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:
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
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
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 halope. Br J Pharmacol 143 960 PMID: 15533888
Lin et al (2019) Functional roles of ST8SIA3-mediated sialylation of striatal DA D2 and adenosine A2A receptors. Transl Psychiatry 9 209 PMID: 31455764
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
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
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
Billes et al (2012) Leptin reduces food intake via a DA D2 receptor-dependent mechanism. Mol Metab 1 86 PMID: 24024122
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.
Dopamine Receptors Scientific Review
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
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.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.