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Submit Review(S)-WAY 100135 dihydrochloride
Description: Potent and selective 5-HT1A antagonist
Chemical Name: (S)-N-tert-Butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide dihydrochloride
Purity: ≥99% (HPLC)
Biological Activity for (S)-WAY 100135 dihydrochloride
(S)-WAY 100135 dihydrochloride is a potent, selective 5-HT1A receptor antagonist (IC50 = 15 nM). Selective over 5-HT1B, 1C, 2,α1, α2 and D2 receptors (IC50 > 1000 nM). Centrally active on systemic administration.
Licensing Information
Sold with the permission of Wyeth-Ayerst Research, US Patent 4,988,814
Compound Libraries for (S)-WAY 100135 dihydrochloride
(S)-WAY 100135 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for (S)-WAY 100135 dihydrochloride
| M. Wt | 468.47 |
| Formula | C24H33N3O2.2HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 149007-54-5 |
| PubChem ID | 6604839 |
| InChI Key | NYZFUZCCDOSQBG-AWEZNQCLSA-N |
| Smiles | O=C(NC(C)(C)C)[C@@]([C@]3=CC=CC=C3)([H])CN(CC2)CCN2C1=C(OC)C=CC=C1.Cl.Cl |
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 (S)-WAY 100135 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.85 | 100 | |
| water | 2.34 | 5 with gentle warming | |
| water | 4.68 | 10 with sonication |
Preparing Stock Solutions for (S)-WAY 100135 dihydrochloride
The following data is based on the product molecular weight 468.47. 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 | 2.13 mL | 10.67 mL | 21.35 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.27 mL |
| 10 mM | 0.21 mL | 1.07 mL | 2.13 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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Product Datasheets for (S)-WAY 100135 dihydrochloride
References for (S)-WAY 100135 dihydrochloride
References are publications that support the biological activity of the product.
Cliffe et al (1993) (S)-N-tert-Butyl-3(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors. J.Med.Chem. 36 1509 PMID: 8496920
Fletcher et al (1993) WAY100135: a novel, selective antagonist at presynaptic and postsynaptic 5-HT1A receptors. Eur.J.Pharmacol. 237 283 PMID: 8365456
Fletcher et al (1993) Silent 5-HT1A receptor antagonists: utility as research tools and therapeutic agents. Trends Pharmacol.Sci. 14 41 PMID: 8122313
Rodgers and Cole (1994) Anxiolytic-like effect of (S)-WAY 100135, a 5-HT1A receptor antagonist, in the murine elevated plus-maze test. Eur.J.Pharmacol. 261 321 PMID: 7813555
If you know of a relevant reference for (S)-WAY 100135 dihydrochloride, please let us know.
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Keywords: (S)-WAY 100135 dihydrochloride, (S)-WAY 100135 dihydrochloride supplier, Potent, selective, 5-HT1A, antagonist, Serotonin, Receptors, (S)-WAY100135, dihydrochloride, 1253, Tocris Bioscience
7 Citations for (S)-WAY 100135 dihydrochloride
Citations are publications that use Tocris products. Selected citations for (S)-WAY 100135 dihydrochloride include:
Pandya and Yakel (2013) Activation of the α7 nicotinic ACh receptor induces anxiogenic effects in rats which is blocked by a 5-HT?a receptor antagonist. Neuropharmacology 70 35 PMID: 23321689
Saxena et al (2013) Neuroprotection through excitability and mTOR required in ALS motoneurons to delay disease and extend survival. Neuron 80 80 PMID: 24094105
Borroto-Escuela et al (2012) The existence of FGFR1-5-HT1A receptor heterocomplexes in midbrain 5-HT neurons of the rat: relevance for neuroplasticity. J Neurosci 32 6295 PMID: 22553035
Grace et al (2012) 5-HT1A receptor-responsive pedunculopontine tegmental neurons suppress REM sleep and respiratory motor activity. J Neurosci 32 1622 PMID: 22302804
Foong et al (2010) 5-HT(1A), SST(1), and SST(2) receptors mediate inhibitory postsynaptic potentials in the submucous plexus of the guinea pig ileum. J Neurosci 298 G384 PMID: 20007849
Chambers et al (2011) Multiple neural oscillators and muscle feedback are required for the intestinal fed state motor program. PLoS One 6 e19597 PMID: 21573176
Hampson et al (2007) Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs. Diabetologia 50 1743 PMID: 17579833
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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.
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.
Depression Poster
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 Poster
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.