8-OH-DPAT
Based on 8 publication(s) in Google Scholar
8-OH-DPAT is a potent, brain-penetrant and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 78950-78-4
- Formula: C16H25NO
- Molecular Weight:247.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) 8-OH-DPAT
More- Nature. 2024 Jun;630(8015):237-246. [Abstract]
- Acta Pharmacol Sin. 2025 Oct 9. [Abstract]
- J Ethnopharmacol. 2026 Feb 28:357:120876. [Abstract]
- Eur J Pharmacol. 2023 Dec 5:960:176147. [Abstract]
- Mol Neurobiol. 2025 Nov 24;63(1):163. [Abstract]
- Neurochem Int. 2025 Jan 28:105937. [Abstract]
- patent. US20260034119A1.
- SSRN. 2025 Jun 19.
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
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT1A Receptor |
5-HT1B Receptor |
5-HT7 Receptor |
5-HT1A Receptor 8.19 (pIC50) |
5-HT7 Receptor 466 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
10.9 nM
Compound: 8-OH-DPAT
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In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
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[PMID: 15887953] |
| CHO | EC50 |
2.6 nM
Compound: 8-OH-DPAT
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In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
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[PMID: 15887953] |
| CHO | EC50 |
26 nM
Compound: 8-OH-DPAT
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Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
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[PMID: 18834188] |
| CHO | EC50 |
15 nM
Compound: 8-OH-DPAT
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Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
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[PMID: 23279866] |
| CHO | IC50 |
5.2 nM
Compound: 8-OH-DPAT
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Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand
Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand
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[PMID: 8759642] |
| CHO | EC50 |
260 nM
Compound: 5
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The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
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[PMID: 9871775] |
| HEK293 | IC50 |
6 nM
Compound: 8-OH-DPAT
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Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells
Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells
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[PMID: 24262884] |
| HEK293 | IC50 |
5.3 x 10-10 M
Compound: 8-OH-DPAT
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Displacement of [3H]8-OHDPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells
Displacement of [3H]8-OHDPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells
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[PMID: 26988801] |
| HEK293 | IC50 |
5.3 x 10-10 M
Compound: 8-OH-DPAT
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Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
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[PMID: 27876250] |
| HEK293 | EC50 |
6 nM
Compound: 8-OH-DPAT
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Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay
Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay
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[PMID: 31547945] |
| HeLa | EC50 |
8 nM
Compound: 8-OH-DPAT
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Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
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[PMID: 24050112] |
| HeLa | EC50 |
0.018 μM
Compound: 8-OH-DPAT
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Compound was evaluated for inhibition of forskolin-stimulated adenylyl cyclase in dose dependent manner in HeLa cells transfected with 5-HTIA
Compound was evaluated for inhibition of forskolin-stimulated adenylyl cyclase in dose dependent manner in HeLa cells transfected with 5-HTIA
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[PMID: 9871719] |
8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A; weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5)[1].
8-OH-DPAT has high affinity at 5-HT7 with a Ki of 466 nM, and does not bind to 5-HT6 or 5-HT4[2].
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.
Chemical Information
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CAS No. 78950-78-4
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Appearance Solid
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Molecular Weight 247.38
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Formula C16H25NO
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Color White to light brown
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SMILES
OC1=C2CC(N(CCC)CCC)CCC2=CC=C1
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Synonyms
8-Hydroxy-DPAT
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Nature
2024 Jun;630(8015):237-246. PMID: 38720072 -
Acta Pharmacol Sin
Esflurbiprofen exerts a fast-onset antidepressant effect by blocking SERT-nNOS interaction. [Abstract]2025 Oct 9. PMID: 41068287
8-OH-DPAT purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2025 Oct 9. [Abstract]
Microinjecting 8-OH-DPAT (4 mM) into the dorsal raphe nucleus (DRN), followed by esflurbiprofen treatment (20 mg/kg, intraperitoneally) at 5 min. TST (F (3, 28) = 6.237, P = 0.0022), FST (F (3, 28) = 4.385, P = 0.0119) were performed 2 h post treatment (n = 8). The results showed that 8-OH-DPAT, a selective 5-HT₁A receptor agonist, abolished the rapid antidepressant activity of esflurbiprofen, confirming that esflurbiprofen exerted antidepressant effects by inhibiting the negative feedback mediated by 5-HT₁A autoreceptors.
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J Ethnopharmacol
The allyl isothiocyanate (AITC) isolated from mustard (Sinapis alba L.) oil exerts antidepressant effects by blocking the interaction between SERT and nNOS. [Abstract]2026 Feb 28:357:120876. PMID: 41274522
8-OH-DPAT purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2026 Feb 28:357:120876. [Abstract]
Microinjecting 8-OH-DPAT (4 mM) into the dorsal raphe nucleus (DRN) followed by AITC ME treatment. TST (F (3,28) = 3.435, P = 0.0303, n = 8) and FST (F (3,28) = 14.79, P < 0.0001, n = 8) were performed 2 h later. The results showed that 8-OH-DPAT, a 5-HT₁AR agonist, abolished the antidepressant activity of AITC ME, indicating that the antidepressant effect of AITC ME was associated with the autoreceptor-mediated negative feedback mechanism of 5-HT₁AR in the DRN.
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Eur J Pharmacol
2023 Dec 5:960:176147. PMID: 37871763 -
Mol Neurobiol
Presence of Astrocytic S1R/5-HT1A Heterocomplex in the mPFC: A Putative Link to S1R Activation Mediated Faster Antidepressant-Like Effects. [Abstract]2025 Nov 24;63(1):163. PMID: 41284099
8-OH-DPAT purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2025 Nov 24;63(1):163. [Abstract]
Co-administration of the sigma-1 receptor (S1R) agonist SA-4503 (1 mg/kg, i.p.) and the 5-HT₁A receptor agonist 8-OH-DPAT (0.3 mg/kg, i.p.) produced synergistic anxiolytic- and antidepressant-like effects.
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Neurochem Int
Sigma-1 receptor activation produces faster antidepressant-like effect through enhancement of hippocampal neuroplasticity: Focus on sigma-1-5-HT1A heteroreceptor complex. [Abstract]2025 Jan 28:105937. PMID: 39884578
8-OH-DPAT purchased from MedChemExpress. Usage Cited in: Neurochem Int. 2025 Jan 28:105937. [Abstract]
Statistical analysis of the percentage of c-Fos+ TPH2+ cells in the experimental groups of mice (n = 6, with samples from at least three mice per group). The results showed that treatment with SA-4503 (1.0 mg/kg; p.o. ; once daily for 3 days), alone or in combination with 8-OH-DPAT (0.3 mg/kg ; i.g.; once daily for 3 days), activated a greater number of serotonergic neurons in the DRN of mice subjected to CRS. Similarly, the combined treatment significantly enhanced the effect of 8-OH-DPAT alone (P = 0.0022).
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Solvent & Solubility
DMSO : 100 mg/mL (404.24 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 5 mg/mL (20.21 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (20.21 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Protocol
Mice[3]
The locomotor activity of mice is measured by an infrared sensor placed in individual home cages. To compare the locomotor activity in the light and dark periods, locomotor activity is monitored at 30-min intervals starting at 8:00 a.m. and 8:00 p.m., respectively. To measure the effects of psychostimulants (8-OH-DPAT, 1, 3 mg/kg, s.c; etc.) on locomotor activity in the dark period, all drugs are administered at 8:00 p.m., and locomotor activity is then measured through 3 h[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (297 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[2]. Bard JA, et al. Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. J Biol Chem. 1993 Nov 5;268(31):23422-6. [Content Brief]
[3]. Mori T, et al. Narcolepsy-like sleep disturbance in orexin knockout mice are normalized by the 5-HT1A receptor agonist 8-OH-DPAT. Psychopharmacology (Berl). 2016 Jun;233(12):2343-53. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.0424 mL | 20.2118 mL | 40.4236 mL | 101.0591 mL |
| 5 mM | 0.8085 mL | 4.0424 mL | 8.0847 mL | 20.2118 mL | |
| 10 mM | 0.4042 mL | 2.0212 mL | 4.0424 mL | 10.1059 mL | |
| 15 mM | 0.2695 mL | 1.3475 mL | 2.6949 mL | 6.7373 mL | |
| 20 mM | 0.2021 mL | 1.0106 mL | 2.0212 mL | 5.0530 mL | |
| 25 mM | 0.1617 mL | 0.8085 mL | 1.6169 mL | 4.0424 mL | |
| 30 mM | 0.1347 mL | 0.6737 mL | 1.3475 mL | 3.3686 mL | |
| 40 mM | 0.1011 mL | 0.5053 mL | 1.0106 mL | 2.5265 mL | |
| 50 mM | 0.0808 mL | 0.4042 mL | 0.8085 mL | 2.0212 mL | |
| 60 mM | 0.0674 mL | 0.3369 mL | 0.6737 mL | 1.6843 mL | |
| 80 mM | 0.0505 mL | 0.2526 mL | 0.5053 mL | 1.2632 mL | |
| 100 mM | 0.0404 mL | 0.2021 mL | 0.4042 mL | 1.0106 mL |
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