WAY-100635
Based on 12 publication(s) in Google Scholar
WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 162760-96-5
- Formula: C25H34N4O2
- Molecular Weight:422.56
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Storage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) WAY-100635
More- Nat Neurosci. 2022 Jan;25(1):39-49. [Abstract]
- Br J Pharmacol. 2026 Feb 27. [Abstract]
- Neuropsychopharmacology. 2026 Feb 13. [Abstract]
- Chin Med. 2024 Jun 15;19(1):87. [Abstract]
- Int Immunopharmacol. 2024 Feb 15:128:111524. [Abstract]
- Neuropharmacology. 2026 Jul 1:292:110950. [Abstract]
- iScience. 2025 Nov 25;28(12):114211. [Abstract]
- Biomedicines. 2025 Sep 23;13(10):2319. [Abstract]
- Psychopharmacology (Berl). 2024 Nov;241(11):2315-2330. [Abstract]
- Psychopharmacology (Berl). 2022 Nov;239(11):3551-3565. [Abstract]
- Cereb Cortex. 2024 Oct 3;34(10):bhae399. [Abstract]
- Chin J Integr Med. 2021 Jul;27(7):534-541. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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RT-PCR
All 5-HT Receptor Isoforms
MoreAll Dopamine Receptor Isoforms
More
Biological Activity
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D4 Receptor |
5-HT1A Receptor |
5-HT1A Receptor 8.87 (pIC50) |
5-HT1A Receptor 9.71 (pA2) |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
7.1 nM
Compound: 1
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Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
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[PMID: 15239661] |
| CHO | EC50 |
7.1 nM
Compound: 1
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Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
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[PMID: 15239661] |
| CHO | IC50 |
7.1 nM
Compound: 4, WAY-100635
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Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
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[PMID: 20443629] |
| HEK293-EBNA | IC50 |
0.91 nM
Compound: 1, WAY-100635
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Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting
Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting
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[PMID: 21520940] |
| JAR | IC50 |
>4500 nM
Compound: 1
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Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells
Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells
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[PMID: 15239661] |
The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D2L or D4.4 receptors[1].
WAY-100635 displays 940, 370, and 16 nM binding affinities at D2L, D3, and D4.2 receptors, respectively. Saturation analyses demonstrat that the Kd of [3H] WAY-100635 at D4.2 receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D4.4 cells with EC50 of 9.7 nM. WAY-100635 possesses high affinity for D4.4 receptor (3.3 nM) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (220-240 g)[2]
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Dosage:1 mg/kg
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Administration:Subcutaneous injection (Pharmacokinetic study)
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Result:Reduced total abstinence score, increased immobility time and the burying behavior was increased.
Chemical Information
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CAS No. 162760-96-5
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Appearance Solid-Liquid Mixture
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Molecular Weight 422.56
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Formula C25H34N4O2
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Color Off-white to light yellow
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SMILES
O=C(N(C1=NC=CC=C1)CCN2CCN(CC2)C3=CC=CC=C3OC)C4CCCCC4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (12)
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Journal Impact Factor
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Most Recent
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Nat Neurosci
Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties. [Abstract]2022 Jan;25(1):39-49. PMID: 34887590 -
Br J Pharmacol
5-HT2A receptors in the prelimbic cortex VIP-expressing interneurons: A mechanism for psychedelic-induced innate fear attenuation. [Abstract]2026 Feb 27. PMID: 41761564 -
Neuropsychopharmacology
Psilocybin improves novel object recognition in a rat model of Fragile X Syndrome through the modulation of the BDNF/TrkB signaling pathway. [Abstract]2026 Feb 13. PMID: 41688761 -
Chin Med
Shaoyao Decoction reduced T lymphocyte activation by regulating of intestinal flora and 5-hydroxytryptamine metabolism in ulcerative colitis. [Abstract]2024 Jun 15;19(1):87. PMID: 38879471
WAY-100635 purchased from MedChemExpress. Usage Cited in: Chin Med. 2024 Jun 15;19(1):87. [Abstract]
5-HT promoted the inflammation in H9 cells. NC, negative control; 5-HT: 5-HT (10 μM) treatment; Way: 5-HT (10 μM) and Way100635 (10 μM) treatment; Tro: 5-HT (10 μM) and Tropisetron (25 μM) treatment; Way + Tro: 5-HT (10 μM), Way100635 (10 μM) and Tropisetron (25 μM) treatment.
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Int Immunopharmacol
Hypidone hydrochloride (YL-0919) protects mice from meningitis via Sigma1R-STAT1-NLRP3-GSDMD pathway. [Abstract]2024 Feb 15:128:111524. PMID: 38232537 -
Neuropharmacology
Novel mechanism of hypidone hydrochloride (YL-0919) in Parkinson's disease: inhibiting neuronal ferroptosis by targeting the Sigma1R-PI3K-AKT-ACSL4 axis. [Abstract]2026 Jul 1:292:110950. PMID: 41887568 -
iScience
Oxygen-dependent regulation of serotonin receptor 5-HT 1A in hypoxic response and flight performance in bumblebees, Bombus terrestris. [Abstract]2025 Nov 25;28(12):114211. PMID: 41384043
WAY-100635 purchased from MedChemExpress. Usage Cited in: iScience. 2025 Nov 25;28(12):114211. [Abstract]
Experimental design for in vivo functional validation of 5-HT1A. 5-HT1A activity was inhibited by injection of 5-HT1A antagonist, WAY-100635.
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Biomedicines
5-Hydroxytryptophan, a Precursor for Serotonin Synthesis, Alleviated Cognitive Dysfunction in a Mouse Model of Sepsis-Associated Encephalopathy. [Abstract]2025 Sep 23;13(10):2319. PMID: 41153606
WAY-100635 purchased from MedChemExpress. Usage Cited in: Biomedicines. 2025 Sep 23;13(10):2319. [Abstract]
Effects of 5-HTP (10 mg/kg) and WAY100635 (1 mg/kg) on cognitive behavior and motor functions in healthy mice. The BM performance (learning and probe trials) across groups.
WAY-100635 purchased from MedChemExpress. Usage Cited in: Biomedicines. 2025 Sep 23;13(10):2319. [Abstract]
Effects of 5-HTP (10 mg/kg) and WAY100635 (1 mg/kg) on cognitive behavior and motor functions in healthy mice. NORT discrimination index across group.
WAY-100635 purchased from MedChemExpress. Usage Cited in: Biomedicines. 2025 Sep 23;13(10):2319. [Abstract]
Impact of WAY100635 pretreatment on 5-HTP's effects in LPS-induced SAE model. Performance during learning phase of BM between groups.
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Psychopharmacology (Berl)
5-hydroxytryptamine 2C/1A receptors modulate the biphasic dose response of the head twitch response and locomotor activity induced by DOM in mice. [Abstract]2024 Nov;241(11):2315-2330. PMID: 38916640 -
Psychopharmacology (Berl)
Contrasting effects of DOI and lisuride on impulsive decision-making in delay discounting task. [Abstract]2022 Nov;239(11):3551-3565. PMID: 36107207 -
Cereb Cortex
A circuit from lateral hypothalamic to dorsal hippocampal dentate gyrus modulates behavioral despair in mice. [Abstract]2024 Oct 3;34(10):bhae399. PMID: 39367727 -
Chin J Integr Med
Combination of Geniposide and Eleutheroside B Exerts Antidepressant-like Effect on Lipopolysaccharide-Induced Depression Mice Model. [Abstract]2021 Jul;27(7):534-541. PMID: 31784933
Solvent & Solubility
DMSO : 66.67 mg/mL (157.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Chemel BR, et al. WAY-100635 is a potent dopamine D4 receptor agonist. Psychopharmacology (Berl). 2006 Oct;188(2):244-51. [Content Brief]
[2]. Mannucci C, et al. Serotonin involvement in Rhodiola rosea attenuation of nicotine withdrawal signs in rats. Phytomedicine. 2012 Sep 15;19(12):1117-24. [Content Brief]
[3]. Al Hussainy R, et al. Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinatedanalogues 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 Med Chem. 2011 May 26;54(10):3480-91. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3665 mL | 11.8326 mL | 23.6653 mL | 59.1632 mL |
| 5 mM | 0.4733 mL | 2.3665 mL | 4.7331 mL | 11.8326 mL | |
| 10 mM | 0.2367 mL | 1.1833 mL | 2.3665 mL | 5.9163 mL | |
| 15 mM | 0.1578 mL | 0.7888 mL | 1.5777 mL | 3.9442 mL | |
| 20 mM | 0.1183 mL | 0.5916 mL | 1.1833 mL | 2.9582 mL | |
| 25 mM | 0.0947 mL | 0.4733 mL | 0.9466 mL | 2.3665 mL | |
| 30 mM | 0.0789 mL | 0.3944 mL | 0.7888 mL | 1.9721 mL | |
| 40 mM | 0.0592 mL | 0.2958 mL | 0.5916 mL | 1.4791 mL | |
| 50 mM | 0.0473 mL | 0.2367 mL | 0.4733 mL | 1.1833 mL | |
| 60 mM | 0.0394 mL | 0.1972 mL | 0.3944 mL | 0.9861 mL | |
| 80 mM | 0.0296 mL | 0.1479 mL | 0.2958 mL | 0.7395 mL | |
| 100 mM | 0.0237 mL | 0.1183 mL | 0.2367 mL | 0.5916 mL |
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