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WAY 100635 maleate
Potent, silent antagonist of 5-HT1A receptors (IC50 = 2.2 nM; Ki = 0.84 nM for rat 5-HT1A receptors). Displays 100-fold selectivity for 5-HT1A over other 5-HT subtypes. Also exhibits agonist activity at dopamine D4 receptors.
|Storage||Desiccate 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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 538.64. 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|
|0.25 mM||7.43 mL||37.13 mL||74.26 mL|
|1.25 mM||1.49 mL||7.43 mL||14.85 mL|
|2.5 mM||0.74 mL||3.71 mL||7.43 mL|
|12.5 mM||0.15 mL||0.74 mL||1.49 mL|
References are publications that support the biological activity of the product.
Mensonides-Harsema et al (2000) Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. J.Med.Chem. 43 432 PMID: 10669570
Zhuang et al (1994) Synthesis and evaluation of 4-(2'-methoxyphenyl)-1-[2'-[N-(2''-pyridinyl)-p-iodobenzamido]ethyl]piperazine (p-MPPI): a new iodinated 5-HT1A ligand. J.Med.Chem. 37 1406 PMID: 8182697
Forster et al (1995) A pharmacological profile of the selective silent 5-HT1A receptor antagonist, WAY-100635. Eur.J.Pharmacol. 281 81 PMID: 8566121
Chemel et al (2006) WAY-100635 is a potent DA D4 receptor agonist. Psychopharmacology (Berl). 188 244 PMID: 16915381
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Keywords: WAY 100635 maleate, WAY 100635 maleate supplier, WAY100635, maleate, 5-ht1a, serotonin, serotonergics, selective, antagonists, dopamine, D4, dopaminergics, 5-HT1A, Receptors, 4380, Tocris Bioscience
7 Citations for WAY 100635 maleate
Citations are publications that use Tocris products. Selected citations for WAY 100635 maleate include:
Wierońska et al (2015) The antipsychotic-like effects in rodents of the positive allosteric modulator Lu AF21934 involve 5-HT1A receptor signaling: mechanistic studies. Sci Transl Med 232 259 PMID: 25012236
Greene et al (2009) Vascular endothelial growth factor signaling is required for the behavioral actions of antidepressant treatment: pharmacological and cellular characterization. Neuropsychopharmacology 34 2459 PMID: 19553916
Yin et al (2017) Selective Modulation of Axonal Sodium Channel Subtypes by 5-HT1A Receptor in Cortical Pyramidal Neuron. Cereb Cortex 27 509 PMID: 26494800
Shimizu et al (2017) Brain serotoninergic nervous system is involved in bombesin-induced frequent urination through brain 5-HT7 receptors in rats. Br J Pharmacol 174 3072 PMID: 28675470
Rodríguez-Muñoz et al (2018) Cannabidiol enhances MOR antinociception, diminishes NMDA-mediated seizures and reduces stroke damage via the sigma 1 receptor. Mol Brain 11 51 PMID: 30223868
Walory et al (2018) Oncotoxic Properties of Serotonin Transporter Inhibitors and 5-HT1A Receptor Ligands. Int J Mol Sci 19 PMID: 30347827
Rawls et al (2010) 5-HT(1A)-like receptor activation inhibits abstinence-induced metha. withdrawal in planarians. Neurosci Lett 484 113 PMID: 20709144
Do you know of a great paper that uses WAY 100635 maleate from Tocris? Please let us know.
Reviews for WAY 100635 maleate
Average Rating: 5 (Based on 1 Review.)
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Used this for validation of a molecular target during behavioral testing in rats. This was used to selectively block central 5-HT1A receptors. Dissolved in water at a dose of 0.5 mg/ ml and 1.0 mg/ml and injected subcutaneously in rats. Injections were followed by behavioral testing.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
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.