WAY-100635 (Synonyms: WAY 100635; WAY100635) |
Catalog No.GC10108
One-Click Copy Product Info
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WAY-100635 is a highly potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91nM and a Ki value of 0.39nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 162760-96-5
Sample solution is provided at 25 µL, 10mM.
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WAY-100635 is a highly potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91nM and a Ki value of 0.39nM[1,2]. The 5-HT1A receptor is widely distributed in the central nervous system (e.g., hippocampus, amygdala) and peripheral nervous tissues (e.g., enteric nerves and cardiovascular system), playing a crucial role in regulating emotional states and the secretion of various hormones[3]. WAY-100635 is also a potent full agonist of the dopamine D4 receptor and is commonly used in positron emission tomography (PET) imaging, neuroscience, and behavioral and cognitive studies[4].
In vitro, pretreatment of human neuroblastoma SH-SY5Y cells with WAY-100635 (10μM) for 1h significantly inhibited the increase in cell viability induced by co-treatment with the antidepressant fluoxetine (1μM) and Aβo (5μM) for 24h[5]. In rat hippocampal homogenates, incubation with WAY-100635 (0.2μM) together with the 5-HT1A receptor agonist (+)-5-Me-8-OH-DPAT for 20min completely blocked the inhibition of forskolin-stimulated cAMP production induced by (+)-5-Me-8-OH-DPAT[6].
In vivo, subcutaneous injection of WAY-100635 (0.1mg/kg) in Albino Swiss mice 15min before treatment completely blocked the hypothermic effect induced by the 5-HT1A receptor agonist 8-OH-DPAT (5mg/kg)[7]. Intraperitoneal injection of WAY-100635 (0.1, 0.2, 0.4mg/kg) in chronic constriction injury (CCI) model mice receiving chrysin treatment dose-dependently reversed the alleviating effects of chrysin on heat hyperalgesia and mechanical allodynia[8].
References:
[1] FORNAL C A, METZLER C W, GALLEGOS R A, et al. WAY-100635, a potent and selective 5-hydroxytryptamine1A antagonist, increases serotonergic neuronal activity in behaving cats: comparison with (S)-WAY-100135[J]. The Journal of pharmacology and experimental therapeutics, 1996, 278(2): 752-762.
[2] AL HUSSAINY R, VERBEEK J, VAN DER BORN D, et al. Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl) piperazin-1-yl] ethyl}-N-(pyridin-2-yl) cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor[J]. Journal of medicinal chemistry, 2011, 54(10): 3480-3491.
[3] SAVITZ J, LUCKI I, DREVETS W C. 5-HT1A receptor function in major depressive disorder[J]. Progress in neurobiology, 2009, 88(1): 17-31.
[4] CLIFFE I A. A retrospect on the discovery of WAY-100635 and the prospect for improved 5-HT1A receptor PET radioligands[J]. Nuclear medicine and biology, 2000, 27(5): 441-447.
[5] YAMAMOTO K, TSUJI M, OGUCHI T, et al. Comparison of Protective Effects of Antidepressants Mediated by Serotonin Receptor in Aβ-Oligomer-Induced Neurotoxicity[J]. Biomedicines, 2024, 12(6): 1158.
[6] TRILLAT A C, MALAGIÉ I, MATHÉ-ALLAINMAT M, et al. Effects of WAY 100635 and (-)-5-Me-8-OH-DPAT, a novel 5-HT1A receptor antagonist, on 8-OH-DPAT responses[J]. European journal of pharmacology, 1998, 347(1): 41-49.
[7] WESOLOWSKA A, BORYCZ J, PALUCHOWSKA M H, et al. Pharmacological analysis of the hypothermic effects of NAN-190 and its analogs, postsynaptic 5-HT1A receptor antagonists, in mice[J]. Polish journal of pharmacology, 2002, 54(4): 391-399.
[8] WU J, WANG Y, CUI W, et al. 5-HT1A receptor-mediated attenuation of heat hyperalgesia and mechanical allodynia by chrysin in mice with experimental mononeuropathy[J]. Regional Anesthesia & Pain Medicine, 2020, 45(8): 610-619.
| Cell experiment [1]: | |
Cell lines | SH-SY5Y cells (human neuroblastoma) |
Preparation Method | SH-SY5Y cells were pretreated with 10μM WAY-100635 for 1h and incubated with 1μM fluoxetine and 5μM Aβo for 24h, then cell viability was assessed using the 3-(4, 5-dimethylthiazoyl-2-yl)-2-5, diphenyltetrazolium bromide (MTT) assay using the MTT Cell Count Kit. |
Reaction Conditions | 10μM; 1h |
Applications | WAY-100635 pretreatment significantly inhibited the increase in cell viability induced by the antidepressant fluoxetine combined with Aβo treatment. |
| Animal experiment [2]: | |
Animal models | Chronic constriction injury (CCI) C57BL/6J mice |
Preparation Method | CCI model mice that received oral Chrysin (30mg/kg; twice a day) for 2 weeks were given a single intraperitoneal injection of WAY-100635 (0.1, 0.2, 0.4 mg/kg) 30min before the scheduled Chrysin administration on the day of behavioral testing, followed by oral Chrysin administration as scheduled 30min later, and then behavioral assessments were performed. |
Dosage form | 0.1, 0.2, 0.4mg/kg; i.p. |
Applications | WAY-100635 treatment dose-dependently reversed the relieving effect of Chrysin on thermal hyperalgesia and mechanical dysphagia. |
References: | |
| Cas No. | 162760-96-5 | SDF | |
| Synonyms | WAY 100635; WAY100635 | ||
| Chemical Name | N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexanecarboxamide | ||
| Canonical SMILES | COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4 | ||
| Formula | C25H34N4O2 | M.Wt | 422.56 |
| Solubility | ≥ 42.3 mg/mL in DMSO, ≥ 134.2 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3665 mL | 11.8326 mL | 23.6653 mL |
| 5 mM | 473.3 μL | 2.3665 mL | 4.7331 mL |
| 10 mM | 236.7 μL | 1.1833 mL | 2.3665 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)