8-OH-DPAT (Synonyms: 8-Hydroxy-DPAT)

Name: 8-OH-DPAT
Brand: MedChemExpress
SKU: HY-112061
Rating: 5.0 (8 reviews)

Cat. No.: HY-112061 Purity: 99.87%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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).

For research use only. We do not sell to patients.

CAS No. : 78950-78-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of 8-OH-DPAT:

8 Publications Citing Use of MCE 8-OH-DPAT

In Vivo Efficacy Study

: 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.

: 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.

: 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.

: 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).

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT Receptor 5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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)

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	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	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	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]
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]
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]
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	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]
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]
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]

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.

Molecular Weight

247.38

Formula

C₁₆H₂₅NO

CAS No.

78950-78-4

Appearance

Solid

Color

White to light brown

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.87%

Select Batch:

Data Sheet (297 KB) SDS (251 KB)

COA (250 KB) HNMR (246 KB) RP-HPLC (243 KB)

Handling Instructions (2659 KB)

References

[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]

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].

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

References

[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]

Complete Stock Solution Preparation Table

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

8-OH-DPAT Related Classifications

Neurological Disease Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

8-OH-DPAT78950-78-48-Hydroxy-DPAT5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

8-OH-DPAT (Synonyms: 8-Hydroxy-DPAT)

Customer Review

Other Forms of 8-OH-DPAT:

8-OH-DPAT Related Antibodies

8 Publications Citing Use of MCE 8-OH-DPAT

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

8-OH-DPAT Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

8-OH-DPAT Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report