Cat. No.: HY-112061

8-OH-DPAT

(Synonyms: 8-Hydroxy-DPAT)

9 Cited Publications

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Based on 9 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 K_i of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC₅₀, 5.42), 5-HT (pIC₅₀ <5).

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Pureté: 99.87%
CAS No.: 78950-78-4
Formule: C₁₆H₂₅NO
Masse moléculaire:247.38

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

8-OH-DPAT Chemical Structure

CAS No.: 78950-78-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

5-HT_1A Receptor

5-HT_1B Receptor

5-HT₇ Receptor

5-HT_1A Receptor

8.19 (pIC₅₀)

5-HT₇ Receptor

466 nM (Ki)

Voir tous les produits spécifiques à Isoform 5-HT Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	10.9 nM Compound: 8-OH-DPAT	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	[PMID: 15887953]
CHO	EC₅₀	2.6 nM Compound: 8-OH-DPAT	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	[PMID: 15887953]
CHO	EC₅₀	26 nM Compound: 8-OH-DPAT	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	[PMID: 18834188]
CHO	EC₅₀	15 nM Compound: 8-OH-DPAT	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	[PMID: 23279866]
CHO	IC₅₀	5.2 nM Compound: 8-OH-DPAT	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	[PMID: 8759642]
CHO	EC₅₀	260 nM Compound: 5	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	[PMID: 9871775]
HEK293	IC₅₀	6 nM Compound: 8-OH-DPAT	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	[PMID: 24262884]
HEK293	IC₅₀	5.3 x 10^-10 M Compound: 8-OH-DPAT	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	[PMID: 26988801]
HEK293	IC₅₀	5.3 x 10^-10 M Compound: 8-OH-DPAT	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	[PMID: 27876250]
HEK293	EC₅₀	6 nM Compound: 8-OH-DPAT	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	[PMID: 31547945]
HeLa	EC₅₀	8 nM Compound: 8-OH-DPAT	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	[PMID: 24050112]
HeLa	EC₅₀	0.018 μM Compound: 8-OH-DPAT	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	[PMID: 9871719]

In Vitro

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 K_i 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.

In Vivo

8-OH-DPAT (1 mg/kg) normalizes hypolocomotion, significantly increases wakefulness and reduces the duration of REM sleep without effect on the duration of non-REM sleep in the dark period in orexin knockout (KO) mice. 8-OH-DPAT shows no obvious effect on wakefulness or the duration of either REM sleep or non-REM sleep in WT mice. 8-OH-DPAT (1 mg/kg, s.c.) activates 5-HT1A receptor in orexin knockout mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 78950-78-4
Appearance Solid
Masse moléculaire 247.38
Formule C₁₆H₂₅NO
Color White to light brown
SMILES

OC1=C2CC(N(CCC)CCC)CCC2=CC=C1
Synonyms

8-Hydroxy-DPAT
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

All In Vivo Efficacy Study

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Journal Impact Factor

Nature

Structural pharmacology and therapeutic potential of 5-methoxytryptamines. [Abstract]

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.
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.
Eur J Pharmacol

Xanthotoxol relieves itch in mice via suppressing spinal GRP/GRPR signaling. [Abstract]

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.
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 Mar:184:105937. PMID: 39884578

8-OH-DPAT purchased from MedChemExpress. Usage Cited in: Neurochem Int. 2025 Mar:184:105937. [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).
Neuropharmacology

Antidepressant-like activity of JZ-1201 in male rodents: a novel selective 5-HT/NE reuptake inhibitor and 5-HT1A receptor partial agonist. [Abstract]

2026 Nov 1:298:111009. PMID: 42107524
patent

US20260034119A1.
SSRN

2025 Jun 19.

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.0424 mL

20.2118 mL

40.4236 mL

5 mM

0.8085 mL

4.0424 mL

8.0847 mL

10 mM

0.4042 mL

2.0212 mL

4.0424 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (20.21 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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

Protocole

Animal Administration^[3]

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.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (297 KB)
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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. DEREK N. MIDDLEMISS, et al. 8-HYDROXY-2-(DI-n-PROPYLAMINO)-TETRALIN DISCRIMINATES BETWEEN SUBTYPES OF

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

8-OH-DPAT

9 Cited Publications

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8-OH-DPAT

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Obesity Compound Library

Antidepressant Compound Library

5-HT Receptor Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

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Membrane Receptor-targeted Compound Library

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Mass Spectrometry Human Metabolite Library

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GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Publications Citing Use of MedChemExpress (MCE) 8-OH-DPAT

Voir tous les produits spécifiques à Isoform 5-HT Receptor

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

8-OH-DPAT

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Obesity Compound Library

Antidepressant Compound Library

5-HT Receptor Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Publications Citing Use of MedChemExpress (MCE) 8-OH-DPAT

Voir tous les produits spécifiques à Isoform 5-HT Receptor

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

8-OH-DPAT Related Classifications

HY-112061 Related Classifications